Cyclosporin A (Synonyms: 环孢素; Cyclosporine A; Ciclosporin A; CsA)

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Cyclosporin A (Cyclosporine A) 是一种免疫抑制剂，能与亲环素结合，抑制 protein phosphatase 2B (PP2B/calcineurin) 活性的IC₅₀ 值为 7 nM。Cyclosporin A 也抑制 CD11a/CD18 粘附分子。

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Cyclosporin A Chemical Structure

CAS No. : 59865-13-3

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥572	In-stock
100 mg	￥520	In-stock
200 mg	￥750	In-stock
500 mg	￥1380	In-stock
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Other Forms of Cyclosporin A:

MCE 顾客使用本产品发表的 119 篇科研文献

Proliferation Assay

: Cyclosporin A purchased from MCE. Usage Cited in: Exp Mol Med. 2022 Feb;54(2):129-142. [Abstract]; Representative western blotting images of cGAS and STING in the Cyclosporine (CsA; 10 μM; for 24 h)- or DMSO-treated NP cells.

: Cyclosporin A purchased from MCE. Usage Cited in: Exp Mol Med. 2022 Feb;54(2):129-142. [Abstract]; Representative western blotting images of NLRP3, ASC, pro-CASP-1, cleaved CASP-1, GSDMD, and cleaved GSDMD in the (CsA; 10 μM; for 24 h)- or DMSO-treated NP cells.

: Cyclosporin A purchased from MCE. Usage Cited in: Exp Mol Med. 2022 Feb;54(2):129-142. [Abstract]; Representative immunofluorescence images of STING with different degrees of polymerization in the Cyclosporine (CsA; 10 μM; for 24 h)- or DMSO-treated NP cells.

: Cyclosporin A purchased from MCE. Usage Cited in: Redox Biol. 2022 Aug;54:102355.; Cells are treated with or without Cyclosporine A (CsA; 2 μM) for 4 h in presence of NRC-03 (45 μg/mL). TUNEL immunofluorescence staining and quantification of TUNEL positive cells.

: Cyclosporin A purchased from MCE. Usage Cited in: Redox Biol. 2022 Aug;54:102355.; Cells are treated with or without Cyclosporine A (CsA; 2 μM) for 4 h in presence of NRC-03 (45 μg/mL). Cell viability determined by CCK-8.

: Cyclosporin A purchased from MCE. Usage Cited in: Aging Dis. 2022 Oct 1;13(5):1546-1561. [Abstract]; Additionally, similar to P-gp siRNA silence, pharmacological inhibition of P-gp with Cyclosporine A (CsA; 22 mg/kg) significantly attenuates P-gp expression levels in ischemic brain as compared to vehicle treatment.

: Cyclosporin A purchased from MCE. Usage Cited in: Nat Commun. 2021 May 18;12(1):2915. [Abstract]; Immunoblot analysis of Cytochrome c from cytosolic extracts and mitochondria from indicated cells pre-treated with DMSO or Cyclosporine A (50 μM) for 1 h, followed with PFOS treatment (150 μM, 6 h).

: Cyclosporin A purchased from MCE. Usage Cited in: Cell Rep. 2021 Nov 30;37(9):110069. [Abstract]; Colony formation of CRC cells treated with Cyclosporine A (CsA; 2.5-5 μM) in combination with 5-FU or OXA for 48 h.

: Cyclosporin A purchased from MCE. Usage Cited in: Cell Rep. 2021 Nov 30;37(9):110069. [Abstract]; Immunoblotting analysis of indicated apoptotic markers expression in CRC cells treated with Cyclosporine A (CsA; 2.5-5 μM) in combination with 5-FU or OXA.

: Cyclosporin A purchased from MCE. Usage Cited in: Cell Death Dis. 2021 Apr 20;12(5):413. [Abstract]; Inhibition of NR-induced increase of co-localized puncta (LC3 and TOM20) after 1 μMCyclosporin A (CsA) pretreatment.

: Cyclosporin A purchased from MCE. Usage Cited in: Cell Death Dis. 2021 Apr 1;12(4):336. [Abstract]; Immunofluorescence staining of subcellular localization of NFATC1 in RANK overexpression and control cells with or without treatment of 10 μg/mL Cyclosporin A (CsA).

: Cyclosporin A purchased from MCE. Usage Cited in: Proc Natl Acad Sci U S A. 2021 Jan 12;118(2):e2009539118. [Abstract]; Calcineurin activities of the PCE after FK506 or Cyclosporine A (CsA; 4 µM) treatment Zebrafish.

: Cyclosporin A purchased from MCE. Usage Cited in: Br J Pharmacol. 2021 Jun;178(11):2305-2323. [Abstract]; Smooth muscle cells are treated cyclosporin A (CsA, 1 μM) or PDTC (10 μM) for 24 h before measuring the activity of PPARγ2 promoter.

: Cyclosporin A purchased from MCE. Usage Cited in: Cell Death Dis. 2018 May 22;9(6):598. [Abstract]; A549 cells are pretreated with 5 µM Cyclosporin A (CSA) for 2 h, followed by treatment with 80 μM Hirsutine for 24 h. equal amount of lysates are subjected to immunoprecipitation using anti-ANT1 antibody, the associated CypD is determined using immunoblotting.

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC₅₀ of 5 nM^[3]. Cyclosporin A also inhibits CD11a/CD18 adhesion^[8].

IC₅₀ & Target

Cyclophilin D

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
2008	IC₅₀	2.7 μM Compound: Cyclosporine A	Inhibition of MRP1 in human 2008 cells assessed as Calcein AM accumulation treated 30 mins before Calcein AM addition measured up to 90 mins by fluorescence assay Inhibition of MRP1 in human 2008 cells assessed as Calcein AM accumulation treated 30 mins before Calcein AM addition measured up to 90 mins by fluorescence assay	[PMID: 24184213]
2008	IC₅₀	2.81 μM Compound: CsA	Inhibition of MRP1 (unknown origin) expressed in human 2008 cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay Inhibition of MRP1 (unknown origin) expressed in human 2008 cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay	[PMID: 23851114]
A2780	GI₅₀	8.94 μM Compound: Cyclosporine A	Cytotoxicity against human A2780 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human A2780 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 27100033]
A2780 ADR	IC₅₀	0.919 μM Compound: CsA	Inhibition of ABCB1 in human A2780adr cells pre-incubated for 30 mins followed by calcein AM addition and further incubated for 60 mins by calcein AM assay Inhibition of ABCB1 in human A2780adr cells pre-incubated for 30 mins followed by calcein AM addition and further incubated for 60 mins by calcein AM assay	[PMID: 25855895]
A2780 ADR	IC₅₀	0.92 μM Compound: Cyclosporine A	Inhibition of MDR1 in human doxorubicin-resistant A2780adr cells assessed as Calcein AM accumulation treated 30 mins before Calcein AM addition measured up to 90 mins by fluorescence assay Inhibition of MDR1 in human doxorubicin-resistant A2780adr cells assessed as Calcein AM accumulation treated 30 mins before Calcein AM addition measured up to 90 mins by fluorescence assay	[PMID: 24184213]
A2780 ADR	IC₅₀	0.99 μM Compound: CsA	Inhibition of p-glycoprotein (unknown origin) expressed in human A2780Adr cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay Inhibition of p-glycoprotein (unknown origin) expressed in human A2780Adr cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay	[PMID: 23851114]
A2780 ADR	IC₅₀	1.21 μM Compound: Cyclosporine A	Inhibition of ABCB1 in human A2780/ADR cells assessed as reduction in calcien-AM efflux preincubated for 30 mins followed by calcien-AM addition measured immediately at 60 sec time interval for 60 mins by fluorescence assay Inhibition of ABCB1 in human A2780/ADR cells assessed as reduction in calcien-AM efflux preincubated for 30 mins followed by calcien-AM addition measured immediately at 60 sec time interval for 60 mins by fluorescence assay	[PMID: 27676469]
A2780 ADR	IC₅₀	1.4 μM Compound: Cyclosporin A	Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780/ADR cells by calcein AM assay Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780/ADR cells by calcein AM assay	[PMID: 19250834]
A2780 ADR	IC₅₀	1.41 μM Compound: Cyclosporine A	Inhibition of ABCB1 in human A2780/ADR cells incubated for 30 mins measured up to 3600 secs with time intervals of 60 secs by calcein accumulation assay Inhibition of ABCB1 in human A2780/ADR cells incubated for 30 mins measured up to 3600 secs with time intervals of 60 secs by calcein accumulation assay	[PMID: 27100033]
A2780 ADR	GI₅₀	8.63 μM Compound: Cyclosporine A	Cytotoxicity against human A2780/ADR cells overexpressing ABCB1 assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human A2780/ADR cells overexpressing ABCB1 assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 27100033]
B-cell	IC₅₀	0.07 μg/mL Compound: cyclosporin A	Immunosuppressive activity in BALB/c mouse splenic B lymphocytes assessed as inhibition of LPS-induced cell proliferation after 72 hrs by MTT assay Immunosuppressive activity in BALB/c mouse splenic B lymphocytes assessed as inhibition of LPS-induced cell proliferation after 72 hrs by MTT assay	[PMID: 14738397]
B-cell	IC₅₀	0.74 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse splenocytes assessed as reduction in LPS-induced mouse B-lymphocytes proliferation incubated for 8 hrs by beta scintillation counting based [3H]thymidine incorporation assay Immunosuppressive activity in BALB/c mouse splenocytes assessed as reduction in LPS-induced mouse B-lymphocytes proliferation incubated for 8 hrs by beta scintillation counting based [3H]thymidine incorporation assay	[PMID: 35678710]
Breast cancer cell line	EC₅₀	0.5 μM Compound: Cyclosporin A	Concentration that reduces the difference in reversal of DOX accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%. Concentration that reduces the difference in reversal of DOX accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%.	[PMID: 11784143]
Breast cancer cell line	EC₅₀	0.6 μM Compound: Cyclosporin A	Concentration that reduces difference in reversal of [3H]VBL accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50% Concentration that reduces difference in reversal of [3H]VBL accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%	[PMID: 11784143]
CCRF-CEM	IC₅₀	3.4 μM Compound: 1	Inhibitory activity against Human MDR1 P-Glycoprotein ABC Transporter using leukemia CEM cells Inhibitory activity against Human MDR1 P-Glycoprotein ABC Transporter using leukemia CEM cells	[PMID: 12361387]
HEK293	IC₅₀	0.7 μM Compound: Cyclosporine A	Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate	[PMID: 22587986]
HEK293	IC₅₀	0.7 μM Compound: Cyclosporine A	Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate	[PMID: 22587986]
HEK293	IC₅₀	1.2 μM Compound: Cyclosporine A	Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate	[PMID: 22587986]
HEK293	IC₅₀	1.3 μM Compound: Cyclosporin A	Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting	[PMID: 22541068]
HEK293	IC₅₀	1.4 μM Compound: Cyclosporin A	Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting	[PMID: 22541068]
HEK293	IC₅₀	37 μM Compound: Cyclosporin A	Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting	[PMID: 22541068]
HeLa	IC₅₀	6.6 μM Compound: Cs	Antiviral activity against HPV-18 infected in human HeLa cells assessed as inhibition of viral replication after 3 days Antiviral activity against HPV-18 infected in human HeLa cells assessed as inhibition of viral replication after 3 days	[PMID: 18212100]
HFF	IC₅₀	> 10000 nM Compound: CSA	Inhibition of fetal calf serum-induced proliferation of human foreskin fibroblast assessed as [3H]thymidine incorporation after 4 days by scintillation counting Inhibition of fetal calf serum-induced proliferation of human foreskin fibroblast assessed as [3H]thymidine incorporation after 4 days by scintillation counting	[PMID: 14593182]
Huh-5-2	EC₅₀	0.3 μM Compound: Cyclosporine A	Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh5-2 cells assessed as reduction in replicon RNA after 4 days by luciferase assay Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh5-2 cells assessed as reduction in replicon RNA after 4 days by luciferase assay	[PMID: 18625766]
Huh-5-2	EC₅₀	306 nM Compound: CsA	Antiviral activity against Hepatitis C virus genotype 1b I389luc-ubi-neo/NS3-3'/5.1 subgenomic replicon infected in human Huh5-2 cells after 4 days by luciferase assay Antiviral activity against Hepatitis C virus genotype 1b I389luc-ubi-neo/NS3-3'/5.1 subgenomic replicon infected in human Huh5-2 cells after 4 days by luciferase assay	10.1039/C1MD00227A
Huh-5-2	CC₅₀	4.4 μM Compound: CsA	Cytostatic activity against human Huh5-2 cells assessed as decrease in cell proliferation after 3 days by MTS method Cytostatic activity against human Huh5-2 cells assessed as decrease in cell proliferation after 3 days by MTS method	10.1039/C1MD00227A
Huh-5-2	CC₅₀	6 μM Compound: Cyclosporine A	Cytotoxicity against human Huh5-2 cells after 3 days by MTT assay Cytotoxicity against human Huh5-2 cells after 3 days by MTT assay	[PMID: 18625766]
Huh-7	EC₅₀	> 10 μM Compound: CsA	Antiviral activity against cyclosporine A/NIM-resistant HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay Antiviral activity against cyclosporine A/NIM-resistant HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay	[PMID: 20176894]
Huh-7	EC₅₀	0.21 μM Compound: CsA	Antiviral activity against HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay Antiviral activity against HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay	[PMID: 20176894]
Huh-7	EC₅₀	137 nM Compound: CsA	Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human Huh7 cells assessed as decrease in subgenomic RNA level after 72 hrs by RT-PCR analysis Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human Huh7 cells assessed as decrease in subgenomic RNA level after 72 hrs by RT-PCR analysis	10.1039/C1MD00227A
Huh-7	EC₅₀	198 nM Compound: CsA	Antiviral activity against Hepatitis C virus genotype 1a H77 infected in human Huh7 cells assessed as decrease in subgenomic RNA level after 72 hrs by RT-PCR analysis Antiviral activity against Hepatitis C virus genotype 1a H77 infected in human Huh7 cells assessed as decrease in subgenomic RNA level after 72 hrs by RT-PCR analysis	10.1039/C1MD00227A
Huh-7	EC₅₀	3.39 μM Compound: CsA	Antiviral activity against cyclosporine A-resistant HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay Antiviral activity against cyclosporine A-resistant HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay	[PMID: 20176894]
Huh-7	EC₅₀	455 nM Compound: CsA	Antiviral activity against Hepatitis C virus genotype 2a JFH-1 infected in human Huh7 cells assessed as decrease in subgenomic RNA level after 72 hrs by RT-PCR analysis Antiviral activity against Hepatitis C virus genotype 2a JFH-1 infected in human Huh7 cells assessed as decrease in subgenomic RNA level after 72 hrs by RT-PCR analysis	10.1039/C1MD00227A
Huh-7	CC₅₀	5.62 μM Compound: CsA	Antiviral activity against Hepatitis C virus infected in human Huh7ET cells assessed as inhibition of viral replication after 72 hrs by luciferase reporter gene assay Antiviral activity against Hepatitis C virus infected in human Huh7ET cells assessed as inhibition of viral replication after 72 hrs by luciferase reporter gene assay	[PMID: 19933795]
Jurkat	IC₅₀	> 10 μM Compound: CsA	Cytotoxicity against human Jurkat cells after 4 days by MTT assay Cytotoxicity against human Jurkat cells after 4 days by MTT assay	[PMID: 22984987]
Jurkat	EC₅₀	0.005 μM Compound: CsA	Antiinflammatory activity in human Jurkat cells assessed as inhibition of anti-CD3/CD28 antibody-induced IL-2 production treated for 1 hr before anti-CD3/CD28 antibody challenge measured after 6 hrs by immunosuppression assay Antiinflammatory activity in human Jurkat cells assessed as inhibition of anti-CD3/CD28 antibody-induced IL-2 production treated for 1 hr before anti-CD3/CD28 antibody challenge measured after 6 hrs by immunosuppression assay	[PMID: 19933795]
Jurkat	IC₅₀	1.4 nM Compound: 1	Inhibition of NFAT activation in PMA/ionomycin-stimulated human Jurkat T cells incubated for 30 mins prior to PMA/ionomycin stimulation measured after 5 hrs by luciferase reporter gene assay Inhibition of NFAT activation in PMA/ionomycin-stimulated human Jurkat T cells incubated for 30 mins prior to PMA/ionomycin stimulation measured after 5 hrs by luciferase reporter gene assay	[PMID: 23964991]
Jurkat	IC₅₀	1.9 μM Compound: CsA	Immunosuppressive activity in human Jurkat cells assessed as reduction in PHA + PMA-induced IL-2 production after 48 hrs by ELISA Immunosuppressive activity in human Jurkat cells assessed as reduction in PHA + PMA-induced IL-2 production after 48 hrs by ELISA	[PMID: 30579802]
Jurkat	IC₅₀	11 nM Compound: 1; CyA	Immunosuppressive activity in human PMA/ionomycin stimulated Jurkat T cells assessed as suppression of IL2 production pretreated with cells followed by PMA/ionomycin stimulation measured after 13 hrs by ELISA Immunosuppressive activity in human PMA/ionomycin stimulated Jurkat T cells assessed as suppression of IL2 production pretreated with cells followed by PMA/ionomycin stimulation measured after 13 hrs by ELISA	[PMID: 27647370]
Jurkat	IC₅₀	12 nM Compound: CsA	The compound was tested in vitro for inhibition of IL-2 release stimulated with PMA/ionomycin by Jurkat cells. The compound was tested in vitro for inhibition of IL-2 release stimulated with PMA/ionomycin by Jurkat cells.	[PMID: 7473543]
Jurkat	IC₅₀	2 nM Compound: CsA	Immunosuppressive activity was measured by inhibition of the IL-2 production in Jurkat cells. Immunosuppressive activity was measured by inhibition of the IL-2 production in Jurkat cells.	[PMID: 14643337]
K562/R7	IC₅₀	0.7 μM Compound: cyclosporin A	Potentiation of doxorubicin-induced cytotoxicity against doxorubicin-resistant human K562/R7 cells assessed as doxorubicin IC50 at 1 uM after 72 hrs by MTT assay Potentiation of doxorubicin-induced cytotoxicity against doxorubicin-resistant human K562/R7 cells assessed as doxorubicin IC50 at 1 uM after 72 hrs by MTT assay	[PMID: 25634041]
KB	IC₅₀	0.6 μM Compound: CSA (cyclosporin A)	Inhibitory activity against KB cell line after 72 h of drug exposure Inhibitory activity against KB cell line after 72 h of drug exposure	[PMID: 15481991]
KB 3-1	IC₅₀	1.5 μM Compound: CSA (cyclosporin A)	Inhibitory activity against KB/MDR cell line after 72 hr of drug exposure Inhibitory activity against KB/MDR cell line after 72 hr of drug exposure	[PMID: 15481991]
L929	IC₅₀	29.9 μM Compound: Cyclosporin A	Cytotoxicity against mouse L929 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against mouse L929 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 34597896]
L929	IC₅₀	30 μM Compound: cyclosporin A	Cytotoxicity against mouse L929 cells after 3 days by MTS assay Cytotoxicity against mouse L929 cells after 3 days by MTS assay	[PMID: 25985195]
L929	IC₅₀	33.9 μM Compound: cyclosporine A	Cytotoxicity against mouse L929 cells assessed as growth inhibition after 3 days by MTS assay Cytotoxicity against mouse L929 cells assessed as growth inhibition after 3 days by MTS assay	[PMID: 24171478]
L929	IC₅₀	33.9 μM Compound: 2	Cytotoxicity against mouse L929 cells after 72 hrs Cytotoxicity against mouse L929 cells after 72 hrs	[PMID: 22320402]
LLC-PK1	IC₅₀	0.7 μM Compound: Cyclosporin a	Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
LLC-PK1	IC₅₀	0.8 μM Compound: Cyclosporin a	Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
LLC-PK1	IC₅₀	4.8 μM Compound: Cyclosporin a	Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
Lymphocyte	IC₅₀	0.054 μM Compound: CsA	Immunosuppressive activity in peripheral blood lymphocytes isolated from two individuals assessed as proliferation using [methyl-3H]thymidine by mixed lymphocyte reaction assay Immunosuppressive activity in peripheral blood lymphocytes isolated from two individuals assessed as proliferation using [methyl-3H]thymidine by mixed lymphocyte reaction assay	[PMID: 21171614]
Lymphocyte	IC₅₀	0.054 μM Compound: CsA	Immunosuppressive activity in lymphocytes by mixed lymphocyte reaction assay Immunosuppressive activity in lymphocytes by mixed lymphocyte reaction assay	[PMID: 20064721]
Lymphocyte	IC₅₀	0.2 μg/mL Compound: Cyclosporin A	Immunosuppressive activity in human lymphocytes by mixed lymphocyte reaction assay Immunosuppressive activity in human lymphocytes by mixed lymphocyte reaction assay	[PMID: 3373220]
Lymphocyte	EC₅₀	60 nM Compound: 1, CSA	Immunosuppressive activity in lymphocytes (unknown origin) by mixed lymphocyte reaction assay Immunosuppressive activity in lymphocytes (unknown origin) by mixed lymphocyte reaction assay	[PMID: 24831536]
Lymphocyte	IC₅₀	89 nM Compound: CsA	Immunosuppressive activity in lymphocytes by MLR assay Immunosuppressive activity in lymphocytes by MLR assay	[PMID: 24900866]
MDCK-II	IC₅₀	25.6 μM Compound: Cyclosporine A	Inhibition of ABCC2 (unknown origin) expressed in MDCK2 cells assessed as inhibition of calcein-AM efflux measured after 30 mins in presence of ABCB1 inhibitor GF120918 and ABCC1 inhibitor MK-571 by flow cytometry Inhibition of ABCC2 (unknown origin) expressed in MDCK2 cells assessed as inhibition of calcein-AM efflux measured after 30 mins in presence of ABCB1 inhibitor GF120918 and ABCC1 inhibitor MK-571 by flow cytometry	[PMID: 27393949]
MT4	IC₅₀	> 0.83 μM Compound: Cs	Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect by MTT assay Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect by MTT assay	[PMID: 18212100]
MT4	EC₅₀	450 nM Compound: 1, CsA	Antiviral activity against HIV1 3B infected in human MT4 cells coinfected with HTLV1 assessed as reduction in virus-induced cytopathogenicity after 4 days by MTT assay Antiviral activity against HIV1 3B infected in human MT4 cells coinfected with HTLV1 assessed as reduction in virus-induced cytopathogenicity after 4 days by MTT assay	[PMID: 23849880]
MT4	CC₅₀	5608 nM Compound: CSA	Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 4 to 5 days by cell-titer glo assay Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 4 to 5 days by cell-titer glo assay	[PMID: 30074795]
PBMC	EC₅₀	0.0031 μM Compound: CsA	Antiinflammatory activity in human PBMC assessed as inhibition of anti-CD3/CD28 antibody-induced IL-2 production treated for 1 hr before anti-CD3/CD28 antibody challenge measured after 6 hrs by immunosuppression assay Antiinflammatory activity in human PBMC assessed as inhibition of anti-CD3/CD28 antibody-induced IL-2 production treated for 1 hr before anti-CD3/CD28 antibody challenge measured after 6 hrs by immunosuppression assay	[PMID: 19933795]
PBMC	IC₅₀	0.056 μM Compound: Cs	Antiproliferative activity against mouse PBMC with MLR assessed as inhibition of [3H]thymidine incorporation after 18 hrs Antiproliferative activity against mouse PBMC with MLR assessed as inhibition of [3H]thymidine incorporation after 18 hrs	[PMID: 18212100]
PBMC	IC₅₀	3 nM Compound: CsA	Immunosuppressive activity in human PBMC isolated from two individuals assessed as inhibition of proliferation using [3H]thymidine by mixed lymphocyte reaction assay Immunosuppressive activity in human PBMC isolated from two individuals assessed as inhibition of proliferation using [3H]thymidine by mixed lymphocyte reaction assay	10.1039/C1MD00227A
RD	CC₅₀	> 10 μM Compound: CsA	Cytotoxicity against human RD cells after 24 hrs by WST-1 assay Cytotoxicity against human RD cells after 24 hrs by WST-1 assay	[PMID: 26564266]
RD	EC₅₀	3.66 μM Compound: CsA	Antiviral activity against EV71 infected in RD cells after 24 hrs by luciferase assay Antiviral activity against EV71 infected in RD cells after 24 hrs by luciferase assay	[PMID: 26564266]
Splenocyte	CC₅₀	> 2.5 μM Compound: CsA	Cytotoxicity in BALB/c mouse Splenocyte assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay Cytotoxicity in BALB/c mouse Splenocyte assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay	[PMID: 35104138]
Splenocyte	IC₅₀	0.01 μg/mL Compound: Cyclosporine A	Antiproliferative activity against concanavalin A-stimulated BALB/c mouse splenocytes after 72 hrs by AlamarBlue assay Antiproliferative activity against concanavalin A-stimulated BALB/c mouse splenocytes after 72 hrs by AlamarBlue assay	[PMID: 23167554]
Splenocyte	IC₅₀	0.01 μM Compound: CsA	Immunosuppressive activity in splenocytes assessed as inhibition of concanavalin A-induced proliferation after 48 hrs by [3H]thymidine incorporation assay Immunosuppressive activity in splenocytes assessed as inhibition of concanavalin A-induced proliferation after 48 hrs by [3H]thymidine incorporation assay	[PMID: 19481938]
Splenocyte	EC₅₀	0.03 μM Compound: Cyclosporine A	Immunosuppressive activity in BALB/c mouse splenocyte assessed as reduction in ConA-induced mouse T-lymphocytes proliferation incubated for 48 hrs by MTT assay Immunosuppressive activity in BALB/c mouse splenocyte assessed as reduction in ConA-induced mouse T-lymphocytes proliferation incubated for 48 hrs by MTT assay	[PMID: 36596229]
Splenocyte	IC₅₀	0.03 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse Splenocyte assessed as inhibition of concanavalin A induced T-cell proliferation by [3H]-thymidine incorporation based beta scintillation counter analysis Immunosuppressive activity in BALB/c mouse Splenocyte assessed as inhibition of concanavalin A induced T-cell proliferation by [3H]-thymidine incorporation based beta scintillation counter analysis	[PMID: 35104138]
Splenocyte	IC₅₀	0.04 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of concanavalin A-stimulated T-cell proliferation by measuring [3H]-thymidine uptake preincubated before concanavalin A stimulation for 48 hrs followed by [3H]-thymidine additio Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of concanavalin A-stimulated T-cell proliferation by measuring [3H]-thymidine uptake preincubated before concanavalin A stimulation for 48 hrs followed by [3H]-thymidine additio	[PMID: 31253536]
Splenocyte	IC₅₀	0.04 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of concanavalin A stimulated T-cell proliferation by measuring [3H]-thymidine uptake preincubated for 48 hrs followed by concanavalin A stimulation and [3H]-thymidine addition f Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of concanavalin A stimulated T-cell proliferation by measuring [3H]-thymidine uptake preincubated for 48 hrs followed by concanavalin A stimulation and [3H]-thymidine addition f	[PMID: 30500185]
Splenocyte	IC₅₀	0.07 μM Compound: CsA	Immunosuppressive activity in splenocytes assessed as inhibition of LPS-induced proliferation after 48 hrs by [3H]thymidine incorporation assay Immunosuppressive activity in splenocytes assessed as inhibition of LPS-induced proliferation after 48 hrs by [3H]thymidine incorporation assay	[PMID: 19481938]
Splenocyte	IC₅₀	0.1 μM Compound: Cyclosporin A	Immunosupressive activity in OVA323-339 peptide-stimulated OT-2 T cell receptor transgenic mouse splenocytes assessed as inhibition of T cell proliferation after 3 days by MTT assay Immunosupressive activity in OVA323-339 peptide-stimulated OT-2 T cell receptor transgenic mouse splenocytes assessed as inhibition of T cell proliferation after 3 days by MTT assay	[PMID: 25537268]
Splenocyte	IC₅₀	0.3 μM Compound: Cyclosporine A	Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of concanavalin A-stimulated T-cell proliferation incubated for 48 hrs by MTT assay Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of concanavalin A-stimulated T-cell proliferation incubated for 48 hrs by MTT assay	[PMID: 33544615]
Splenocyte	IC₅₀	0.32 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse Splenocyte assessed as inhibition of LPS induced B-cell proliferation by [3H]-thymidine incorporation based beta scintillation counter analysis Immunosuppressive activity in BALB/c mouse Splenocyte assessed as inhibition of LPS induced B-cell proliferation by [3H]-thymidine incorporation based beta scintillation counter analysis	[PMID: 35104138]
Splenocyte	IC₅₀	0.4 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of LPS-stimulated B-cell proliferation by measuring [3H]-thymidine uptake preincubated before LPS stimulation for 48 hrs followed by [3H]-thymidine addition for 8 hrs by beta-sc Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of LPS-stimulated B-cell proliferation by measuring [3H]-thymidine uptake preincubated before LPS stimulation for 48 hrs followed by [3H]-thymidine addition for 8 hrs by beta-sc	[PMID: 31253536]
Splenocyte	IC₅₀	0.4 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of LPS-stimulated B-cell proliferation by measuring [3H]-thymidine uptake preincubated for 48 hrs followed by LPS stimulation and [3H]-thymidine addition for 8 hrs measured afte Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of LPS-stimulated B-cell proliferation by measuring [3H]-thymidine uptake preincubated for 48 hrs followed by LPS stimulation and [3H]-thymidine addition for 8 hrs measured afte	[PMID: 30500185]
Splenocyte	CC₅₀	0.88 μM Compound: CsA	Cytotoxicity against splenocytes after 48 hrs by MTT assay Cytotoxicity against splenocytes after 48 hrs by MTT assay	[PMID: 19481938]
Splenocyte	CC₅₀	1.2 μM Compound: CsA	Cytotoxicity against BALB/c mouse splenocytes assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay Cytotoxicity against BALB/c mouse splenocytes assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay	[PMID: 31253536]
Splenocyte	CC₅₀	1.2 μM Compound: CsA	Cytotoxicity against BALB/c mouse splenocytes after 48 hrs by CCK-8 assay Cytotoxicity against BALB/c mouse splenocytes after 48 hrs by CCK-8 assay	[PMID: 30500185]
Splenocyte	IC₅₀	10 nM Compound: Cyclosporine A	Immunosuppressive activity in human splenocytes assessed as inhibition of [3H]thymidine incorporation after 4 days by allogenic mixed lymphocyte reaction assay Immunosuppressive activity in human splenocytes assessed as inhibition of [3H]thymidine incorporation after 4 days by allogenic mixed lymphocyte reaction assay	[PMID: 19827831]
Splenocyte	IC₅₀	10.15 μM Compound: CsA	Cytotoxicity against BALB/c mouse splenocyte assessed as reduction in cell viability measured after 72 hrs by CCK-8 assay Cytotoxicity against BALB/c mouse splenocyte assessed as reduction in cell viability measured after 72 hrs by CCK-8 assay	[PMID: 33973788]
Splenocyte	IC₅₀	17 nM Compound: Cyclosporine A	Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of [3H]thymidine incorporation after 4 days by allogenic mixed lymphocyte reaction assay Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of [3H]thymidine incorporation after 4 days by allogenic mixed lymphocyte reaction assay	[PMID: 19827831]
Splenocyte	IC₅₀	30 nM Compound: 1, CsA	Immunosuppressant activity in mouse splenocytes by mixed-leukocyte reaction assay Immunosuppressant activity in mouse splenocytes by mixed-leukocyte reaction assay	[PMID: 23017885]
Splenocyte	CC₅₀	7.33 μM Compound: CsA	Cytotoxicity in BALB/c mouse Splenocyte assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity in BALB/c mouse Splenocyte assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 35678710]
T cell line	IC₅₀	26 nM Compound: CsA	Antiproliferative activity against Con A-induced BALB/c mouse T cell after 48 hrs by CCK8 assay Antiproliferative activity against Con A-induced BALB/c mouse T cell after 48 hrs by CCK8 assay	[PMID: 32822186]
T cell line	CC₅₀	9.8 μM Compound: CsA	Cytotoxicity against BALB/c mouse T cell assessed as reduction in cell viability after 48 hrs by CCK8 assay Cytotoxicity against BALB/c mouse T cell assessed as reduction in cell viability after 48 hrs by CCK8 assay	[PMID: 32822186]
T-cell	IC₅₀	> 10000 nM Compound: CSA	Inhibition of IL2-induced proliferation of human T cells assessed as [3H]thymidine incorporation after 72 hrs by scintillation counting Inhibition of IL2-induced proliferation of human T cells assessed as [3H]thymidine incorporation after 72 hrs by scintillation counting	[PMID: 14593182]
T-cell	IC₅₀	0.011 μM Compound: CsA	Immunosuppressive activity in mouse T cells assessed as inhibition of two way mixed lymphocyte reaction after 4 days by MTT assay Immunosuppressive activity in mouse T cells assessed as inhibition of two way mixed lymphocyte reaction after 4 days by MTT assay	[PMID: 22984987]
T-cell	IC₅₀	0.03 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse splenocytes assessed as reduction in ConA-induced mouse T-lymphocytes proliferation incubated for 8 hrs by beta scintillation counting based [3H]thymidine incorporation assay Immunosuppressive activity in BALB/c mouse splenocytes assessed as reduction in ConA-induced mouse T-lymphocytes proliferation incubated for 8 hrs by beta scintillation counting based [3H]thymidine incorporation assay	[PMID: 35678710]
T-cell	IC₅₀	0.04 μg/mL Compound: cyclosporin A	Immunosuppressive activity in BALB/c mouse splenic T lymphocytes assessed as inhibition of Con A-induced cell proliferation after 72 hrs by MTT assay Immunosuppressive activity in BALB/c mouse splenic T lymphocytes assessed as inhibition of Con A-induced cell proliferation after 72 hrs by MTT assay	[PMID: 14738397]
T-cell	IC₅₀	0.06 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse T cells assessed as inhibition of anti-CD3/anti-CD28-stimulated cell proliferation after 72 hrs by MTT assay Immunosuppressive activity in BALB/c mouse T cells assessed as inhibition of anti-CD3/anti-CD28-stimulated cell proliferation after 72 hrs by MTT assay	[PMID: 21131104]
T-cell	IC₅₀	0.07 μM Compound: CsA	Immunosuppressive activity in lymph node T cell assessed as inhibition of ConA-stimulated cell proliferation after 72 hrs by MTT assay Immunosuppressive activity in lymph node T cell assessed as inhibition of ConA-stimulated cell proliferation after 72 hrs by MTT assay	[PMID: 22300886]
T-cell	IC₅₀	0.08 μM Compound: Cyclosporin A	Inhibition of ConA-induced cell proliferation of BALB/c mouse T-lymphocytes assessed as reduction in [3H]thymidine incorporation incubated for 48 hrs by beta scintillation counting method Inhibition of ConA-induced cell proliferation of BALB/c mouse T-lymphocytes assessed as reduction in [3H]thymidine incorporation incubated for 48 hrs by beta scintillation counting method	[PMID: 28294615]
T-cell	IC₅₀	0.2 μM Compound: CsA	Immunosuppressant activity in human T lymphocytes assessed as inhibition of anti-human CD3 and anti-human CD28 monoclonal antibody-induced T lymphocyte proliferation incubated for 72 hrs by FACS analysis Immunosuppressant activity in human T lymphocytes assessed as inhibition of anti-human CD3 and anti-human CD28 monoclonal antibody-induced T lymphocyte proliferation incubated for 72 hrs by FACS analysis	[PMID: 31181920]
T-cell	IC₅₀	0.34 μM Compound: cyclosporin A	Inhibition of PHA-induced human T cell proliferation after 24 hrs by MTT assay Inhibition of PHA-induced human T cell proliferation after 24 hrs by MTT assay	[PMID: 11678649]
T-cell	CC₅₀	13.78 μM Compound: CsA	Cytotoxicity against lymph node T cell after 24 hrs by MTT assay Cytotoxicity against lymph node T cell after 24 hrs by MTT assay	[PMID: 22300886]
T-cell	IC₅₀	14 nM Compound: cyclosporin A	Immunosuppressive activity in BALB/c/C57BL/6 mouse T cells assessed as inhibition of alloantigen-induced cell proliferation after 96 hrs by measuring [3H]thymidine uptake by mixed lymphocyte reaction assay Immunosuppressive activity in BALB/c/C57BL/6 mouse T cells assessed as inhibition of alloantigen-induced cell proliferation after 96 hrs by measuring [3H]thymidine uptake by mixed lymphocyte reaction assay	[PMID: 21456524]
T-cell	CC₅₀	15.82 μM Compound: CsA	Cytotoxicity against BALB/c mouse T cells after 48 hrs by MTT assay Cytotoxicity against BALB/c mouse T cells after 48 hrs by MTT assay	[PMID: 21131104]
T-cell	IC₅₀	2.12 μM Compound: csa	Immunosuppressive activity in BALB/c mouse T cells assessed as inhibition of ConA-induced T cell proliferation incubated 24 hrs post ConA-induction for 72 hrs by MTT assay Immunosuppressive activity in BALB/c mouse T cells assessed as inhibition of ConA-induced T cell proliferation incubated 24 hrs post ConA-induction for 72 hrs by MTT assay	[PMID: 22727369]
T-cell	IC₅₀	32 nM Compound: CSA	Inhibition of allogenic cells-stimulated proliferation in mouse T cells by mixed lymphocyte reaction method Inhibition of allogenic cells-stimulated proliferation in mouse T cells by mixed lymphocyte reaction method	[PMID: 14593182]
T-cell	CC₅₀	4.5 μM Compound: Cyclosporin A	Cytotoxic activity against BALB/c mouse T-lymphocytes assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxic activity against BALB/c mouse T-lymphocytes assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 28294615]
T-cell	IC₅₀	550 nM Compound: CsA	Immunosuppressive activity in concanavalin A-activated T cell assessed as inhibition of lymphoproliferation after 3 days by beta-scintillation counting Immunosuppressive activity in concanavalin A-activated T cell assessed as inhibition of lymphoproliferation after 3 days by beta-scintillation counting	[PMID: 19502058]
T-cell	EC₅₀	6.4 nM Compound: CsA	Immunosuppressive activity in human PBMC assessed as inhibition of anti-human CD3-induced T-cell proliferation after 4 days by CellTrace violet cell proliferation dye based FACS analysis Immunosuppressive activity in human PBMC assessed as inhibition of anti-human CD3-induced T-cell proliferation after 4 days by CellTrace violet cell proliferation dye based FACS analysis	[PMID: 28075591]
T-cell	IC₅₀	74 nM Compound: CSA	Inhibition of allogenic cells-stimulated proliferation in human T cells by mixed lymphocyte reaction method Inhibition of allogenic cells-stimulated proliferation in human T cells by mixed lymphocyte reaction method	[PMID: 14593182]
Ventricular myocyte	IC₅₀	2 μM Compound: Cyclosporin A	Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes	[PMID: 22761000]
Vero	CC₅₀	> 50 μM Compound: Cyclosporine	Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr	10.1101/2020.03.20.999730
Vero	IC₅₀	≤ 0.5 μM Compound: Cs	Antiviral activity against Dengue virus 1 infected in african green monkey Vero cells assessed as decrease in viral RNA synthesis after 24 hrs by luciferase reporter gene assay Antiviral activity against Dengue virus 1 infected in african green monkey Vero cells assessed as decrease in viral RNA synthesis after 24 hrs by luciferase reporter gene assay	[PMID: 19451286]
Vero	IC₅₀	5.82 μM Compound: Cyclosporine	Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr	10.1101/2020.03.20.999730
Vero	IC₅₀	8 μM Compound: Cs	Antiviral activity against West Nile virus infected in african green monkey Vero cells assessed as decrease in viral RNA synthesis after 24 hrs by luciferase reporter gene assay Antiviral activity against West Nile virus infected in african green monkey Vero cells assessed as decrease in viral RNA synthesis after 24 hrs by luciferase reporter gene assay	[PMID: 19451286]

体外研究
(In Vitro)

Cyclosporin A 能够与 T 细胞中的亲环素结合^[1]。
Cyclosporin A 通过形成 Cyclophilin-Cyclosporin A 复合物来抑制神经钙蛋白^[2]。
Cyclosporin A 抑制受刺激细胞中的神经钙蛋白，IC₅₀ 值为 7 nM^[3]。
Cyclosporin A 抑制 NF-AT 的核转位^[4]。Cyclosporin A 通过阻止 MTP 打开对线粒体产生影响，IC₅₀ 为 39 nM^[5]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Cyclosporin A 可用于构建尿毒症模型，在雄性 Wistar 大鼠（体重140-200 g，年龄 5-6 周）中，静脉给予 Cyclosporin A (10 mg/kg) 后的药代动力学参数显示，曲线下面积为 27.3 μg·h/mL，半衰期为 6.9 小时，分布容积为 3.7 L/kg^[9]。

诱导尿毒症^[10]^[11]

致病原理

Cyclosporin A 给药通过刺激转化生长因子 β (TGF-β) 信号通路诱导 III 型胶原蛋白间质沉积和纤维化，同时通过调节基质金属肽酶 9 抑制细胞外基质 (ECM) 降解，从而导致细胞外基质失衡^[10]。

具体造模方法：

小鼠：6-8 周龄 C57BL/6 小鼠
给药方式：30 mg/kg • 皮下注射 • 每日给药，共 16 周

Note

造模成功指标

代谢变化：尿素氮 (BUN) 水平↑
组织学分析: 肾小管损伤、间质炎症和纤维化。
分子变化: LOX、LOXL2、TNFα、MCP-1、(NOX)4 的 mRNA 表达&uarr，α-SMA，FN，COL1A、MCP-1蛋白表达&uarr。

相关产品： /

拮抗产品： Lipoxygenase, general (HY-P2976); Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11) (HY-P990107)

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

1202.61

Formula

C₆₂H₁₁₁N₁₁O₁₂

CAS 号

59865-13-3

性状

固体

颜色

White to off-white

中文名称

环孢霉素A；环孢素A；环孢多肽A；环孢灵；赛斯平；环孢素

结构分类

Others

初始来源

微生物

the fungus Beauveria nivea.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

细胞实验：

DMSO 中的溶解度 : 62.5 mg/mL (51.97 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

Ethanol 中的溶解度 : 50 mg/mL (41.58 mM; 超声助溶)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.8315 mL	4.1576 mL	8.3152 mL
5 mM	0.1663 mL	0.8315 mL	1.6630 mL
10 mM	0.0832 mL	0.4158 mL	0.8315 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: 2.62 mg/mL (2.18 mM); 悬浊液; 超声助溶
方案二

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.08 mg/mL (1.73 mM); 悬浊液; 超声助溶

此方案可获得 2.08 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案三

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (1.73 mM); 悬浊液; 超声助溶

此方案可获得 2.08 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案四

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (1.73 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

请依序添加每种溶剂： Corn Oil
Solubility: 20 mg/mL (16.63 mM); 澄清溶液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.90%

选择批次：

Data Sheet (672 KB) SDS (419 KB)

COA (298 KB) LCMS (193 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Handschumacher RE, et al. Cyclophilin: a specific cytosolic binding protein for cyclosporin A. Science. 1984 Nov 2;226(4674):544-7. [Content Brief]

[2]. Liu J, et al. Calcineurin is a common target of cyclophilin-cyclosporin A and FKBP-FK506 complexes. Cell. 1991 Aug 23;66(4):807-15. [Content Brief]

[3]. Fruman DA, et al. Calcineurin phosphatase activity in T lymphocytes is inhibited by FK 506 and cyclosporin A. Proc Natl Acad Sci U S A. 1992 May 1;89(9):3686-90. [Content Brief]

[4]. Flanagan WM, et al. Nuclear association of a T-cell transcription factor blocked by FK-506 and cyclosporin A. Nature. 1991 Aug 29;352(6338):803-7. [Content Brief]

[5]. Nicolli A, et al. Interactions of cyclophilin with the mitochondrial inner membrane and regulation of the permeability transition pore, and cyclosporin A-sensitive channel. J Biol Chem. 1996 Jan 26;271(4):2185-92. [Content Brief]

[6]. Borel JF, et al. Effects of the new anti-lymphocytic peptide cyclosporin A in animals. Immunology. 1977 Jun;32(6):1017-25. [Content Brief]

[7]. Williams, R, et al. Randomised trial comparing FK506 and cyclosporin in prevention of liver allograft rejection. European FK506 Multicentre Liver Study Group. Lancet, 1994, 344(8920), 423-428. [Content Brief]

[8]. Dalmarco EM, et al. Cyclosporin A inhibits CD11a/CD18 adhesion molecules due to inhibition of TNFalpha and IL-1 beta levels in the mouse model of pleurisy induced by carrageenan. Cell Adh Migr. 2008 Oct-Dec;2(4):231-5. [Content Brief]

[9]. Medeiros M, et al. Increased cyclosporine bioavailability induced by experimental nephrotic syndrome in rats. Can J Physiol Pharmacol. 2007 May;85(5):502-6. [Content Brief]

[10]. Nguyen LT, et al. Lysyl oxidase inhibitors attenuate cyclosporin A-induced nephropathy in mouse. Sci Rep. 2021 Jun 14;11(1):12437. [Content Brief]

[11]. Ling H, et al. Therapeutic role of TGF-beta-neutralizing antibody in mouse cyclosporin A nephropathy: morphologic improvement associated with functional preservation. J Am Soc Nephrol. 2003 Feb;14(2):377-88. [Content Brief]

Cell Assay ^[3]	Immunosuppressive agents are dissolved in ethanol at concentrations 1000-fold more than the concentration desired for cell treatments. Cells (10⁶) are suspended in 1 mL of complete medium in microcentrifuge tubes; 1 μL of ethanol or of the ethanolic solution of Cyclosporin A is added, and the cells are incubated at 37°C for 1 hr. Cells are washed twice with 1 mL of PBS on ice and lysed in 50 μL of hypotonic buffer containing 50 mM Tris (pH 7.5); 0.1 mM EGTA; 1 mM EDTA; 0.5 mM dithiothreitol; and 50 μg of phenylmethylsulfonyl fluoride, 50 μg of soybean trypsin inhibitor, 5 μg of leupeptin, and 5 μg of Kiker 52G per mL. Lysates are subjected to three cycles of freezing in liquid nitrogen followed by thawing at 30°C and then are centrifuged at 4°C for 10 min at 12,000×g. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[6]	Rats are immunized on day 0 i.p. with 0 5 mL and mice i.v. with 0 2 mL of a 10% suspension of washed sheep erythrocytes (SE). To elicit a secondary response, mice are boosted 8-11 weeks after the primary immunization with an i.v. injection of 0-2 mL of 0 25% washed SE (10⁷ cells). For prolonged treatment the animals receive on the average 45 mg/kg cyclosporin A daily in the food during 13 weeks. These rats are immunized 5 days before killing. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Handschumacher RE, et al. Cyclophilin: a specific cytosolic binding protein for cyclosporin A. Science. 1984 Nov 2;226(4674):544-7. [Content Brief] [2]. Liu J, et al. Calcineurin is a common target of cyclophilin-cyclosporin A and FKBP-FK506 complexes. Cell. 1991 Aug 23;66(4):807-15. [Content Brief] [3]. Fruman DA, et al. Calcineurin phosphatase activity in T lymphocytes is inhibited by FK 506 and cyclosporin A. Proc Natl Acad Sci U S A. 1992 May 1;89(9):3686-90. [Content Brief] [4]. Flanagan WM, et al. Nuclear association of a T-cell transcription factor blocked by FK-506 and cyclosporin A. Nature. 1991 Aug 29;352(6338):803-7. [Content Brief] [5]. Nicolli A, et al. Interactions of cyclophilin with the mitochondrial inner membrane and regulation of the permeability transition pore, and cyclosporin A-sensitive channel. J Biol Chem. 1996 Jan 26;271(4):2185-92. [Content Brief] [6]. Borel JF, et al. Effects of the new anti-lymphocytic peptide cyclosporin A in animals. Immunology. 1977 Jun;32(6):1017-25. [Content Brief] [7]. Williams, R, et al. Randomised trial comparing FK506 and cyclosporin in prevention of liver allograft rejection. European FK506 Multicentre Liver Study Group. Lancet, 1994, 344(8920), 423-428. [Content Brief] [8]. Dalmarco EM, et al. Cyclosporin A inhibits CD11a/CD18 adhesion molecules due to inhibition of TNFalpha and IL-1 beta levels in the mouse model of pleurisy induced by carrageenan. Cell Adh Migr. 2008 Oct-Dec;2(4):231-5. [Content Brief] [9]. Medeiros M, et al. Increased cyclosporine bioavailability induced by experimental nephrotic syndrome in rats. Can J Physiol Pharmacol. 2007 May;85(5):502-6. [Content Brief] [10]. Nguyen LT, et al. Lysyl oxidase inhibitors attenuate cyclosporin A-induced nephropathy in mouse. Sci Rep. 2021 Jun 14;11(1):12437. [Content Brief] [11]. Ling H, et al. Therapeutic role of TGF-beta-neutralizing antibody in mouse cyclosporin A nephropathy: morphologic improvement associated with functional preservation. J Am Soc Nephrol. 2003 Feb;14(2):377-88. [Content Brief]

Cyclosporin A 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

Ethanol / DMSO	1 mM	0.8315 mL	4.1576 mL	8.3152 mL	20.7881 mL
	5 mM	0.1663 mL	0.8315 mL	1.6630 mL	4.1576 mL
	10 mM	0.0832 mL	0.4158 mL	0.8315 mL	2.0788 mL
	15 mM	0.0554 mL	0.2772 mL	0.5543 mL	1.3859 mL
	20 mM	0.0416 mL	0.2079 mL	0.4158 mL	1.0394 mL
	25 mM	0.0333 mL	0.1663 mL	0.3326 mL	0.8315 mL
	30 mM	0.0277 mL	0.1386 mL	0.2772 mL	0.6929 mL
	40 mM	0.0208 mL	0.1039 mL	0.2079 mL	0.5197 mL
DMSO	50 mM	0.0166 mL	0.0832 mL	0.1663 mL	0.4158 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Cyclosporin A59865-13-3Cyclosporine A Ciclosporin A CsA环孢霉素A环孢素A环孢多肽A环孢灵赛斯平环孢素Molecular GluesComplement SystemAntibioticCyclophilinInhibitorinhibitorinhibit

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Cyclosporin A (Synonyms: 环孢素; Cyclosporine A; Ciclosporin A; CsA)

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Cyclosporin A (Synonyms: 环孢素; Cyclosporine A; Ciclosporin A; CsA)

Customer Review

Other Forms of Cyclosporin A:

Cyclosporin A 相关抗体

MCE 顾客使用本产品发表的 119 篇科研文献

Cyclosporin A 相关产品

•相关化合物库:

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•同靶点蛋白产品:

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