1. Anti-infection
  2. Reverse Transcriptase HIV HBV
  3. Tenofovir

Tenofovir  (Synonyms: 替诺福韦; GS 1278; PMPA)

目录号: HY-13910 纯度: 99.89%
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Tenofovir (GS 1278) 是一种核苷酸逆转录酶 (nucleotide reverse transcriptase) 抑制剂,可用于 HIV和慢性乙型肝炎 (Hepatitis B; HBV) 的研究。

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Tenofovir Chemical Structure

Tenofovir Chemical Structure

CAS No. : 147127-20-6

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Other Forms of Tenofovir:

查看 HIV 亚型特异性产品:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Tenofovir (GS 1278) is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B (HBV)[1].

IC50 & Target

HIV-1

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Bone marrow cell CC50
3.5 μM
Compound: 2, TFV
Cytotoxicity against human bone marrow cells after 24 hrs by BFU-E assay
Cytotoxicity against human bone marrow cells after 24 hrs by BFU-E assay
[PMID: 20439609]
Bone marrow cell CC50
4.7 μM
Compound: 2, TFV
Cytotoxicity against human bone marrow cells after 24 hrs by GM-CFU assay
Cytotoxicity against human bone marrow cells after 24 hrs by GM-CFU assay
[PMID: 20439609]
C3H/3T3 EC50
0.23 μM
Compound: (R)-PMPA, Tenofovir
Inhibition of murine sarcoma virus-induced transformation of mouse embryo fibroblast C3H/3T3 cells after 6 days
Inhibition of murine sarcoma virus-induced transformation of mouse embryo fibroblast C3H/3T3 cells after 6 days
[PMID: 18556209]
C8166 EC50
7.1 μM
Compound: (R)-PMPA, Tenofovir
Antiviral activity against 100 TCID50 wild-type Human immunodeficiency virus type 2 ROD infected in C8166 cells assessed as inhibition of syncytia formation after 4 days by microscopic analysis
Antiviral activity against 100 TCID50 wild-type Human immunodeficiency virus type 2 ROD infected in C8166 cells assessed as inhibition of syncytia formation after 4 days by microscopic analysis
[PMID: 21803462]
CCRF-CEM CC50
> 100 μM
Compound: Tenofovir
Cytotoxicity against human CEM cells assessed as cell count after 3 days
Cytotoxicity against human CEM cells assessed as cell count after 3 days
[PMID: 26513643]
CCRF-CEM CC50
> 250 μM
Compound: (R)-PMPA
Cytotoxicity against human CEM cells assessed as inhibition of cell proliferation after 72 hrs by coulter counter analysis
Cytotoxicity against human CEM cells assessed as inhibition of cell proliferation after 72 hrs by coulter counter analysis
[PMID: 21429755]
CCRF-CEM EC50
3.2 μM
Compound: (R)-PMPA
Antiviral activity against HIV2 ROD infected in human CEM cells assessed as inhibition of virus-induced syncytium formation after 4 to 5 days by microscopic analysis
Antiviral activity against HIV2 ROD infected in human CEM cells assessed as inhibition of virus-induced syncytium formation after 4 to 5 days by microscopic analysis
[PMID: 21429755]
CCRF-CEM EC50
3.7 μM
Compound: Tenofovir
Antiviral activity against HIV2 ROD infected in human CEM cells assessed as inhibition of virus-induced giant cell formation after 4 to 5 days by microscopic analysis
Antiviral activity against HIV2 ROD infected in human CEM cells assessed as inhibition of virus-induced giant cell formation after 4 to 5 days by microscopic analysis
[PMID: 26513643]
CCRF-CEM EC50
3.7 μM
Compound: Tenofovir
Antiviral activity against HIV2 ROD infected in human CEM cells assessed as reduction in virus-induced cytopathicity after 4 to 5 days by microscopy based syncytium cell formation assay
Antiviral activity against HIV2 ROD infected in human CEM cells assessed as reduction in virus-induced cytopathicity after 4 to 5 days by microscopy based syncytium cell formation assay
[PMID: 25617695]
CCRF-CEM EC50
3.7 μM
Compound: 2, (R)-PMPA
Antiviral activity against Human immunodeficiency virus type 2 ROD infected in human CEM cells assessed as inhibition of virus-induced giant cell formation after 4 to 5 days by microscopic analysis
Antiviral activity against Human immunodeficiency virus type 2 ROD infected in human CEM cells assessed as inhibition of virus-induced giant cell formation after 4 to 5 days by microscopic analysis
[PMID: 24686012]
CCRF-CEM EC50
3.9 μM
Compound: Tenofovir
Antiviral activity against HIV1 3B infected in human CEM cells assessed as inhibition of virus-induced giant cell formation after 4 to 5 days by microscopic analysis
Antiviral activity against HIV1 3B infected in human CEM cells assessed as inhibition of virus-induced giant cell formation after 4 to 5 days by microscopic analysis
[PMID: 26513643]
CCRF-CEM EC50
3.9 μM
Compound: Tenofovir
Antiviral activity against HIV1 3B infected in human CEM cells assessed as reduction in virus-induced cytopathicity after 4 to 5 days by microscopy based syncytium cell formation assay
Antiviral activity against HIV1 3B infected in human CEM cells assessed as reduction in virus-induced cytopathicity after 4 to 5 days by microscopy based syncytium cell formation assay
[PMID: 25617695]
CCRF-CEM EC50
3.9 μM
Compound: 2, (R)-PMPA
Antiviral activity against Human immunodeficiency virus 1 3B infected in human CEM cells assessed as inhibition of virus-induced giant cell formation after 4 to 5 days by microscopic analysis
Antiviral activity against Human immunodeficiency virus 1 3B infected in human CEM cells assessed as inhibition of virus-induced giant cell formation after 4 to 5 days by microscopic analysis
[PMID: 24686012]
CCRF-CEM EC50
4.1 μM
Compound: (R)-PMPA, Tenofovir
Antiviral activity against 100 TCID50 wild-type Human immunodeficiency virus 1 3B infected in CEM cells assessed as inhibition of syncytia formation after 4 days by microscopic analysis
Antiviral activity against 100 TCID50 wild-type Human immunodeficiency virus 1 3B infected in CEM cells assessed as inhibition of syncytia formation after 4 days by microscopic analysis
[PMID: 21803462]
CCRF-CEM EC50
4.6 μM
Compound: (R)-PMPA
Antiviral activity against HIV1 3B infected in human CEM cells assessed as inhibition of virus-induced syncytium formation after 4 to 5 days by microscopic analysis
Antiviral activity against HIV1 3B infected in human CEM cells assessed as inhibition of virus-induced syncytium formation after 4 to 5 days by microscopic analysis
[PMID: 21429755]
CCRF-CEM IC50
6.9 μM
Compound: 2, (R)-PMPA
Cytostatic activity against human CEM cells after 72 hrs by coulter counting analysis
Cytostatic activity against human CEM cells after 72 hrs by coulter counting analysis
[PMID: 24686012]
CHO CC50
173 μM
Compound: Tenofovir
Ratio of CC50 for CHO cells to CC50 for CHO cells expressing hOAT1 after 120 hrs by Cell-Titer Glo assay
Ratio of CC50 for CHO cells to CC50 for CHO cells expressing hOAT1 after 120 hrs by Cell-Titer Glo assay
[PMID: 19001108]
CHO CC50
21 μM
Compound: Tenofovir
Cytotoxicity against CHO cells after 120 hrs by Cell-Titer Glo assay
Cytotoxicity against CHO cells after 120 hrs by Cell-Titer Glo assay
[PMID: 19001108]
CHO CC50
435 μM
Compound: Tenofovir
Cytotoxicity against CHO cells expressing hOAT1 after 120 hrs by Cell-Titer Glo assay
Cytotoxicity against CHO cells expressing hOAT1 after 120 hrs by Cell-Titer Glo assay
[PMID: 19001108]
H9 CC50
> 100 μM
Compound: (R)-PMPA, Tenofovir
Cytotoxicity against PAP-activated human H9 cells on day 7 by MTT assay
Cytotoxicity against PAP-activated human H9 cells on day 7 by MTT assay
[PMID: 21803462]
H9 EC50
0.23 μM
Compound: (R)-PMPA, Tenofovir
Antiviral activity against 125 TCID50 wild type HIV1 LAI infected in human H9 cells assessed as reduction in viral replication measured on day 7 post infection by reverse transcriptase activity
Antiviral activity against 125 TCID50 wild type HIV1 LAI infected in human H9 cells assessed as reduction in viral replication measured on day 7 post infection by reverse transcriptase activity
[PMID: 21803462]
H9 EC50
8.3 μM
Compound: (R)-PMPA, Tenofovir
Antiviral activity against 6250 TCID50 wild type HIV1 LAI infected in human H9 cells assessed as reduction in viral replication measured on day 7 post infection by reverse transcriptase activity
Antiviral activity against 6250 TCID50 wild type HIV1 LAI infected in human H9 cells assessed as reduction in viral replication measured on day 7 post infection by reverse transcriptase activity
[PMID: 21803462]
HEK-293T CC50
> 100 μM
Compound: PMPA
Cytotoxicity against human 293T cells assessed as inhibition of cell proliferation by tetrazolium dye method
Cytotoxicity against human 293T cells assessed as inhibition of cell proliferation by tetrazolium dye method
[PMID: 17470654]
HEK-293T CC50
> 100 μM
Compound: TFV
Cytotoxicity against HEK293T cells assessed as reduction in cell viability in absence of HSA measured after 48 hrs by CellTiter 96 Aqueous One Solution reagent based cell proliferation assay
Cytotoxicity against HEK293T cells assessed as reduction in cell viability in absence of HSA measured after 48 hrs by CellTiter 96 Aqueous One Solution reagent based cell proliferation assay
[PMID: 34459598]
HEK-293T CC50
35.4 μM
Compound: TFV
Cytotoxicity against HEK293T cells assessed as reduction in cell viability measured after 48 hrs by CellTiter 96 Aqueous One Solution reagent based cell proliferation assay
Cytotoxicity against HEK293T cells assessed as reduction in cell viability measured after 48 hrs by CellTiter 96 Aqueous One Solution reagent based cell proliferation assay
[PMID: 34459598]
HeLa IC50
17 μM
Compound: 2, (R)-PMPA
Cytostatic activity against human HeLa cells after 72 hrs by coulter counting analysis
Cytostatic activity against human HeLa cells after 72 hrs by coulter counting analysis
[PMID: 24686012]
HepG2 CC50
> 100 μM
Compound: PMPA, tenofovir
Cytotoxicity against human HepG2 cells by MTS assay
Cytotoxicity against human HepG2 cells by MTS assay
[PMID: 17646420]
HepG2 IC50
12.3 μM
Compound: PMPA, 2
Antiviral activity against Hepatitis B virus infected human HepG2 cells after 9 days by MTT assay
Antiviral activity against Hepatitis B virus infected human HepG2 cells after 9 days by MTT assay
[PMID: 17888662]
HepG2 2.2.15 CC50
> 1716 μM
Compound: Tf
Cytotoxicity against human HepG2.2.15 cells by MTT assay
Cytotoxicity against human HepG2.2.15 cells by MTT assay
[PMID: 24731274]
HepG2 2.2.15 CC50
> 1740.95 μM
Compound: TF
Cytotoxicity against human HepG2(2.2.15) cells by modified-MTT assay
Cytotoxicity against human HepG2(2.2.15) cells by modified-MTT assay
[PMID: 22687441]
HepG2 2.2.15 IC50
> 1742.2 μM
Compound: Tenofovir
Antiviral activity against hepatitis B viral in human HepG2.2.15 cells assessed as surface antigen HBsAg secretion after 72 hrs by ELISA
Antiviral activity against hepatitis B viral in human HepG2.2.15 cells assessed as surface antigen HBsAg secretion after 72 hrs by ELISA
[PMID: 25737008]
HepG2 2.2.15 IC50
> 1742.2 μM
Compound: Tenofovir
Antiviral activity against hepatitis B viral in human HepG2.2.15 cells assessed as surface antigen HBeAg secretion after 72 hrs by ELISA
Antiviral activity against hepatitis B viral in human HepG2.2.15 cells assessed as surface antigen HBeAg secretion after 72 hrs by ELISA
[PMID: 25737008]
HepG2 2.2.15 CC50
> 1742.2 μM
Compound: Tenofovir
Cytotoxicity against human HepG 2.2.15 cells by MTT assay
Cytotoxicity against human HepG 2.2.15 cells by MTT assay
[PMID: 25737008]
HepG2 2.2.15 CC50
> 1820.42 μM
Compound: TF
Cytotoxicity against human HepG2(2.2.15) cells by MTT assay
Cytotoxicity against human HepG2(2.2.15) cells by MTT assay
[PMID: 22472044]
HepG2 2.2.15 CC50
> 300 μM
Compound: PMPA, tenofovir
Cytotoxicity against human HepG2(2.2.15) cells after 24 hrs by neutral red uptake assay
Cytotoxicity against human HepG2(2.2.15) cells after 24 hrs by neutral red uptake assay
[PMID: 17646420]
HepG2 2.2.15 IC50
0.68 μM
Compound: TF
Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of viral DNA replication by PCR analysis
Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of viral DNA replication by PCR analysis
[PMID: 22687441]
HepG2 2.2.15 IC50
0.77 μM
Compound: TF
Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of viral DNA replication by RT-PCR analysis
Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of viral DNA replication by RT-PCR analysis
[PMID: 22472044]
HepG2 2.2.15 CC50
1.85 mM
Compound: TF
Cytotoxicity against human HepG2(2.2.15) cells after 72 hrs by MTT assay
Cytotoxicity against human HepG2(2.2.15) cells after 72 hrs by MTT assay
[PMID: 25737009]
HepG2 2.2.15 IC50
1160.23 μM
Compound: TF
Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of viral e antigen secretion by ELISA
Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of viral e antigen secretion by ELISA
[PMID: 22687441]
HepG2 2.2.15 IC50
1236.61 μM
Compound: TF
Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as suppression of HbeAg secretion by ELISA
Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as suppression of HbeAg secretion by ELISA
[PMID: 22472044]
HepG2 2.2.15 IC50
1238 μM
Compound: Tf
Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as inhibition of hepatitis B e antigen secretion by ELISA
Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as inhibition of hepatitis B e antigen secretion by ELISA
[PMID: 24731274]
HepG2 2.2.15 IC50
1389 μM
Compound: Tf
Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as inhibition of hepatitis B surface antigen secretion by ELISA
Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as inhibition of hepatitis B surface antigen secretion by ELISA
[PMID: 24731274]
HepG2 2.2.15 IC50
1446.35 μM
Compound: TF
Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as suppression of HBsAg secretion by ELISA
Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as suppression of HBsAg secretion by ELISA
[PMID: 22472044]
HepG2 2.2.15 IC50
1450.11 μM
Compound: TF
Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of viral surface antigen secretion by ELISA
Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of viral surface antigen secretion by ELISA
[PMID: 22687441]
HepG2 2.2.15 IC50
2.9 μM
Compound: Tenofovir
Antiviral activity against hepatitis B viral in human HepG2.2.15 cells assessed as decrease in viral DNA replication treated for 7 days by real time PCR analysis
Antiviral activity against hepatitis B viral in human HepG2.2.15 cells assessed as decrease in viral DNA replication treated for 7 days by real time PCR analysis
[PMID: 25737008]
HepG2 2.2.15 CC50
399 μM
Compound: Tenofovir
Cytotoxicity in human HepG2.215 cells assessed as reduction in cell viability after 5 days by CCK8 assay
Cytotoxicity in human HepG2.215 cells assessed as reduction in cell viability after 5 days by CCK8 assay
[PMID: 28082068]
HepG2 2.2.15 EC50
6.4 x 10-5 μM
Compound: TDF
Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as reduction in viral DNA levels incubated for 6 days by PCR analysis
Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as reduction in viral DNA levels incubated for 6 days by PCR analysis
[PMID: 32421339]
HepG2 2.2.15 EC50
7.2 μM
Compound: PMPA, tenofovir
Antiviral activity against HBV in human HepG2(2.2.15) cells assessed as viral DNA levels treated for 9 days measured after 24 hrs
Antiviral activity against HBV in human HepG2(2.2.15) cells assessed as viral DNA levels treated for 9 days measured after 24 hrs
[PMID: 17646420]
Huh-7 EC50
4.2 μM
Compound: (R)-PMPA, Tenofovir
Antiviral activity against Hepatitis B virus infected in human HuH7 cells assessed as reduction in viral DNA level treated day 3 to day 8 post transfection by real time quantitative PCR analysis
Antiviral activity against Hepatitis B virus infected in human HuH7 cells assessed as reduction in viral DNA level treated day 3 to day 8 post transfection by real time quantitative PCR analysis
[PMID: 21803462]
L1210 IC50
11 μM
Compound: 2, (R)-PMPA
Cytostatic activity against mouse L1210 cells after 48 hrs by coulter counting analysis
Cytostatic activity against mouse L1210 cells after 48 hrs by coulter counting analysis
[PMID: 24686012]
MT2 CC50
> 100 μM
Compound: TFV
Cytotoxicity against human MT2 cells assessed as cell viability by CellTiter Glo assay
Cytotoxicity against human MT2 cells assessed as cell viability by CellTiter Glo assay
[PMID: 34549952]
MT2 CC50
> 1000 μM
Compound: 1, PMPA
Cytotoxicity against human MT2 cells after 5 days
Cytotoxicity against human MT2 cells after 5 days
[PMID: 19179082]
MT2 CC50
> 50000 nM
Compound: 2, PMPA or TFV
Cytotoxicity against human MT2 cells after 5 days by XTT assay
Cytotoxicity against human MT2 cells after 5 days by XTT assay
[PMID: 20409721]
MT2 EC50
0.65 μM
Compound: PMPA, tenofovir
Antiviral activity against HIV1 LAI in human MT2 cells assessed as inhibition of p24 antigen production by ELISA
Antiviral activity against HIV1 LAI in human MT2 cells assessed as inhibition of p24 antigen production by ELISA
[PMID: 17646420]
MT2 EC50
13 nM
Compound: 2, PMPA or TFV
Antiviral activity against HIV1 3B infected in human MT2 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by XTT assay
Antiviral activity against HIV1 3B infected in human MT2 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by XTT assay
[PMID: 20409721]
MT2 EC50
3.6 μM
Compound: 1, PMPA
Antiviral activity against HIV1 3a infected human MT2 cells assessed as inhibition of viral-induced cytopathic effect after 3 days by XTT assay
Antiviral activity against HIV1 3a infected human MT2 cells assessed as inhibition of viral-induced cytopathic effect after 3 days by XTT assay
[PMID: 19179082]
MT2 EC50
3.6 μM
Compound: 2
Inhibition of virus-induced cytopathic effect in wild type HIV 3a infected MT2 cells after 5 days
Inhibition of virus-induced cytopathic effect in wild type HIV 3a infected MT2 cells after 5 days
[PMID: 17562366]
MT2 EC50
5 μM
Compound: Tenofovir
Antiviral activity against HIV1 3B infected in human MT2 cells assessed as protection against virus-induced cytopathic effect after 5 days by XTT assay
Antiviral activity against HIV1 3B infected in human MT2 cells assessed as protection against virus-induced cytopathic effect after 5 days by XTT assay
[PMID: 27748590]
MT4 CC50
> 20 μM
Compound: PMPA
Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 6 days by XTT tetrazolium dye-based assay
Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 6 days by XTT tetrazolium dye-based assay
[PMID: 28682067]
MT4 EC50
0 μM
Compound: TDF
Antiviral activity against X4-HIV1 NL4-3 assessed as inhibition of p24 Gag protein production in human MT4 cells by MTT assay
Antiviral activity against X4-HIV1 NL4-3 assessed as inhibition of p24 Gag protein production in human MT4 cells by MTT assay
[PMID: 17548498]
PBMC CC50
> 100 μM
Compound: (R)-PMPA, Tenofovir
Cytotoxicity against PAP-activated human PBMC on day 7 by MTT assay
Cytotoxicity against PAP-activated human PBMC on day 7 by MTT assay
[PMID: 21803462]
PBMC CC50
> 100 μM
Compound: TFV
Cytotoxicity in uninfected human PBMC assessed as reduction in cell viability by XTT assay
Cytotoxicity in uninfected human PBMC assessed as reduction in cell viability by XTT assay
[PMID: 27933889]
PBMC CC50
> 100 μM
Compound: TFV
Cytotoxicity against human PBMC assessed as reduction in cell viability by XTT assay
Cytotoxicity against human PBMC assessed as reduction in cell viability by XTT assay
[PMID: 27405794]
PBMC CC50
> 25 μM
Compound: PMPA
Cytotoxicity against human PHA-stimulated PBMC assessed as cell viability by tetrazolium dye assay
Cytotoxicity against human PHA-stimulated PBMC assessed as cell viability by tetrazolium dye assay
[PMID: 28682067]
PBMC CC50
≥ 10 μM
Compound: (R)-PMPA; Tenofovir
Cytotoxicity against human PBMC assessed as reduction in cell growth after 7 days by MTT assay
Cytotoxicity against human PBMC assessed as reduction in cell growth after 7 days by MTT assay
[PMID: 29558735]
PBMC CC50
1270 μM
Compound: PMPA, tenofovir
Cytotoxicity against human PBMC by XTT assay
Cytotoxicity against human PBMC by XTT assay
[PMID: 17646420]
PBMC CC50
53 μM
Compound: TDF
Cytotoxicity against human PHA-PBMC cells by MTT assay
Cytotoxicity against human PHA-PBMC cells by MTT assay
[PMID: 17548498]
TZM CC50
> 100 μM
Compound: PMPA
Cytotoxicity against human TZM-bl cells assessed as cell viability by tetrazolium dye assay
Cytotoxicity against human TZM-bl cells assessed as cell viability by tetrazolium dye assay
[PMID: 28682067]
体外研究
(In Vitro)

Tenofovir shows cytotoxic effects on cell viability in HK-2 cells, with IC50 values of 9.21 and 2.77 μM at 48 and 72 h in MTT assay, respectively. Tenofovir diminishes ATP levels in HK-2 cells. Tenofovir (3.0 to 28.8 μM) increases oxidative stress and protein carbonylation in HK-2 cells. Furthermore, Tenofovir induces apoptosis in HK-2 cells, and that apoptosis is induced via mitochondrial damage[1]. Tenofovir and M48U1 formulated in 0.25% HEC each inhibits the replication of both R5-tropic HIV-1BaL and X4-tropic HIV-1IIIb in activated PBMCs, and inhibits several laboratory strains and patient-derived HIV-1 isolates. The combined formulation of M48U1 and tenofovir in 0.25% HEC exhibits synergistic antiretroviral activity against infection with R5-tropic HIV-1BaL, and is not toxic to PBMCs[2].

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

体内研究
(In Vivo)

Tenofovir Disoproxil Fumarate (20, 50, 140, or 300 mg/kg) administered to BLT mice, shows dose dependent activity during vaginal HIV challenge in BLT humanized mice. Tenofovir Disoproxil Fumarate (50, 140, 300 mg/kg) significantly reduces HIV transmission in BLT mice[3]. Tenofovir Disoproxil Fumarate (0.5, 1.5, or 5.0 mg/kg/day, p.o.) induces a dose-dependent decline in serum viremia in woodchucks chronically infected with WHV. Tenofovir Disoproxil Fumarate administration is safe and effective in the woodchuck model of chronic HBV infection[4].

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

Clinical Trial
分子量

287.21

Formula

C9H14N5O4P

CAS 号
性状

固体

颜色

White to off-white

中文名称

替诺福韦;替洛福韦

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 7.69 mg/mL (26.77 mM; 超声助溶 (<80°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

H2O 中的溶解度 : 2 mg/mL (6.96 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 3.4818 mL 17.4089 mL 34.8177 mL
5 mM 0.6964 mL 3.4818 mL 6.9635 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

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: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 0.77 mg/mL (2.68 mM); 澄清溶液

    此方案可获得 ≥ 0.77 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 7.7 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 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 0.77 mg/mL (2.68 mM); 澄清溶液

    此方案可获得 ≥ 0.77 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 7.7 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。

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: PBS

    Solubility: 1.96 mg/mL (6.82 mM); 澄清溶液; 超声助溶 (<60°C)

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

g

每只动物的给药体积

μL

动物数量

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)。
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: 99.89%

参考文献
Cell Assay
[1]

Cells are plated into 48-well tissue culture plates (39,000 cells/mL) and allowed to grow for 48 h followed by treatment with vehicle or Tenofovir. Following the treatment period, cell viability is assessed using the MTT assay. The MTT assay relies on the conversion of tetrazolium dye 3-(4,5-dimethlthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) to formazan by NAD(P)H-dependent oxidoreductases[1].

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

Animal Administration
[4]

Twenty adult chronic WHV carrier woodchucks are stratified equally by age, sex, body weight, and serum GGT activity into five treatment groups consisting of four animals each: (i) Tenofovir Disoproxil Fumarate at 15.0 mg/kg once per day, (ii) Tenofovir Disoproxil Fumarate at 5.0 mg/kg/day, (iii) Tenofovir Disoproxil Fumarate at 1.5 mg/kg/day, (iv) Tenofovir Disoproxil Fumarate at 0.5 mg/kg/day, and (v) a placebo control. The woodchucks are treated daily for 4 weeks and observed for an additional 12 weeks following cessation of drug treatment[4].

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

参考文献

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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 3.4818 mL 17.4089 mL 34.8177 mL 87.0443 mL
5 mM 0.6964 mL 3.4818 mL 6.9635 mL 17.4089 mL
DMSO 10 mM 0.3482 mL 1.7409 mL 3.4818 mL 8.7044 mL
15 mM 0.2321 mL 1.1606 mL 2.3212 mL 5.8030 mL
20 mM 0.1741 mL 0.8704 mL 1.7409 mL 4.3522 mL
25 mM 0.1393 mL 0.6964 mL 1.3927 mL 3.4818 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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.

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