1. Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  2. Drug Metabolite VD/VDR Endogenous Metabolite
  3. Calcitriol

Calcitriol  (Synonyms: 骨化三醇; 1,25-Dihydroxyvitamin D3)

目录号: HY-10002 纯度: 99.94%
COA 产品使用指南

Calcitriol 是活性最大的 vitamin D 代谢物,也是 vitamin D 受体 (VDR) 的激动剂。

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Calcitriol Chemical Structure

Calcitriol Chemical Structure

CAS No. : 32222-06-3

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Customer Review

Other Forms of Calcitriol:

MCE 顾客使用本产品发表的 46 篇科研文献

WB
Proliferation Assay

    Calcitriol purchased from MCE. Usage Cited in: Int Immunopharmacol. 2017 Jun;47:182-189.  [Abstract]

    The total number of sneezing and nasal rubbing motions is significantly reduced by 1,25-(OH)2D3, n=9.

    Calcitriol purchased from MCE. Usage Cited in: Oncotarget. 2017 Oct 26;8(59):100187-100195.  [Abstract]

    Calcitriol increases the expressions of JMJD3 and p16INK4A. 786-O cells are treated with vehicle (Veh) or 100nM Calcitriol (Cal) for 48h, and untreated group as control (Con). The expressions of JMJD3 and p16INK4A are determined with western blotting.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Calcitriol is the most active metabolite of vitamin D and also a vitamin D receptor (VDR) agonist.

    IC50 & Target

    Human Endogenous Metabolite

     

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    Bone marrow cell EC50
    100 nM
    Compound: 1-alpha, 25-(OH)2D3
    Effect on osteoclast formation in ddY mouse bone marrow cells co cultured with primary osteoclasts after 3 days relative to 1-alpha, 25-(OH)2D3
    Effect on osteoclast formation in ddY mouse bone marrow cells co cultured with primary osteoclasts after 3 days relative to 1-alpha, 25-(OH)2D3
    [PMID: 18539034]
    Bone marrow cell EC50
    2 nM
    Compound: 1-alpha, 25-(OH)2D3
    Effect on osteoclast formation in ddY mouse bone marrow cells co cultured with primary osteoclasts after 3 days
    Effect on osteoclast formation in ddY mouse bone marrow cells co cultured with primary osteoclasts after 3 days
    [PMID: 18539034]
    BXPC-3 IC50
    21.07 μM
    Compound: 3; 1,25(OH)2D3
    Antiproliferative activity against human BxPC3 cells after 24 hrs by MTT assay
    Antiproliferative activity against human BxPC3 cells after 24 hrs by MTT assay
    [PMID: 30193216]
    Caco-2 EC50
    223.4 nM
    Compound: 1,25(OH)2D3
    Activation of VDR in human Caco2 cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay
    Activation of VDR in human Caco2 cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay
    [PMID: 27070779]
    Caco-2 IC50
    4.4 μM
    Compound: Calcitriol
    Antipoliferative activity against human Caco2 cells after 48 hrs by MTT assay
    Antipoliferative activity against human Caco2 cells after 48 hrs by MTT assay
    [PMID: 26562542]
    Caco-2 IC50
    4.46 μM
    Compound: Calcitriol
    Antiproliferative activity against human Caco2 cells after 48 hrs by MTT assay
    Antiproliferative activity against human Caco2 cells after 48 hrs by MTT assay
    [PMID: 29518319]
    Caco-2 EC50
    515.2 nM
    Compound: 1,25(OH)2D3
    Transactivation of VDR in human Caco2 cells after 24 hrs by luciferase reporter gene assay
    Transactivation of VDR in human Caco2 cells after 24 hrs by luciferase reporter gene assay
    [PMID: 26367019]
    COS-7 EC50
    50 nM
    Compound: 1, 1,25-(OH)2D3
    Agonist activity at human VDR in COS7 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay
    Agonist activity at human VDR in COS7 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay
    [PMID: 17904370]
    COS-7 EC50
    500 pM
    Compound: 1, 1,25-(OH)2D3
    Induction of transactivation of human VDR responsive gene in COS7 cells by rat osteopontin luciferase reporter gene assay
    Induction of transactivation of human VDR responsive gene in COS7 cells by rat osteopontin luciferase reporter gene assay
    [PMID: 17298045]
    HaCaT EC50
    249.7 nM
    Compound: 1,25(OH)2D3
    Activation of VDR in human HaCaT cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay
    Activation of VDR in human HaCaT cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay
    [PMID: 27070779]
    HaCaT EC50
    321.5 nM
    Compound: 1,25(OH)2D3
    Transactivation of VDR in human HaCaT cells after 24 hrs by luciferase reporter gene assay
    Transactivation of VDR in human HaCaT cells after 24 hrs by luciferase reporter gene assay
    [PMID: 26367019]
    HCT-116 IC50
    0.01 nM
    Compound: 1b, calcitriol
    Cytotoxicity against human HCT116 assessed as decrease in cell count after 120 hrs
    Cytotoxicity against human HCT116 assessed as decrease in cell count after 120 hrs
    [PMID: 22926068]
    HEK293 IC50
    > 10 μM
    Compound: 1, 1,25-VD3
    Antagonist activity at human androgen receptor expressed in HEK293 cells assessed as inhibition of transcriptional activity by luciferase and beta-galactosidase reporter gene assay
    Antagonist activity at human androgen receptor expressed in HEK293 cells assessed as inhibition of transcriptional activity by luciferase and beta-galactosidase reporter gene assay
    [PMID: 23462715]
    HEK293 EC50
    0.003 μM
    Compound: 1, 1,25-VD3
    Agonist activity at CMX-GAL4 tagged human VDR expressed in HEK293 cells assessed as increase in transcriptional activity by luciferase reporter gene assay
    Agonist activity at CMX-GAL4 tagged human VDR expressed in HEK293 cells assessed as increase in transcriptional activity by luciferase reporter gene assay
    [PMID: 23462715]
    HEK293 IC50
    0.1 nM
    Compound: 1; 1,25(OH)2D3
    Agonist activity at VDR (unknown origin) expressed in HEK293 cells cotransfected with NCoR assessed as decrease in NCoR recruitment by two-hybrid assay
    Agonist activity at VDR (unknown origin) expressed in HEK293 cells cotransfected with NCoR assessed as decrease in NCoR recruitment by two-hybrid assay
    [PMID: 26613420]
    HEK293 EC50
    0.12 nM
    Compound: 1; 1,25(OH)2D3
    Agonist activity at VDR in human HEK293 cells assessed as transcriptional activity after 16 to 24 hrs by luciferase reporter gene assay
    Agonist activity at VDR in human HEK293 cells assessed as transcriptional activity after 16 to 24 hrs by luciferase reporter gene assay
    [PMID: 26613420]
    HEK293 EC50
    0.6 nM
    Compound: 1; 1,25(OH)2D3
    Agonist activity at VDR (unknown origin) expressed in HEK293 cells cotransfected with RXRalpha assessed as RXRalpha recruitment by two-hybrid assay
    Agonist activity at VDR (unknown origin) expressed in HEK293 cells cotransfected with RXRalpha assessed as RXRalpha recruitment by two-hybrid assay
    [PMID: 26613420]
    HEK293 EC50
    1 nM
    Compound: 1, 1,25-(OH)2D3
    Agonist activity at human VDR in HEK293 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay
    Agonist activity at human VDR in HEK293 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay
    [PMID: 17904370]
    HEK293 EC50
    7.28 x 10-10 M
    Compound: 1,25(OH)2D3, Calcitriol
    Antiproliferative activity against NHEK cells incubated for 24 hrs by [3H]thymidine incorporation assay
    Antiproliferative activity against NHEK cells incubated for 24 hrs by [3H]thymidine incorporation assay
    [PMID: 22404326]
    HeLa EC50
    1 nM
    Compound: calcitriol, [1alpha,25(OH)2D3]
    Transactivation of GAL4-fused VDR ligand binding domain expressed in human HeLa cells after 16 hrs by luciferase reporter gene assay
    Transactivation of GAL4-fused VDR ligand binding domain expressed in human HeLa cells after 16 hrs by luciferase reporter gene assay
    [PMID: 22957834]
    HeLa EC50
    2.5 nM
    Compound: calcitriol, [1alpha,25(OH)2D3]
    Transactivation of full length human VDR expressed in human HeLa cells assessed as increase in CYP24 transcription after 18 hrs by luciferase reporter gene assay
    Transactivation of full length human VDR expressed in human HeLa cells assessed as increase in CYP24 transcription after 18 hrs by luciferase reporter gene assay
    [PMID: 22957834]
    HepG2 IC50
    > 50 μM
    Compound: Calcitriol
    Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
    Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
    [PMID: 29518319]
    HepG2 IC50
    > 50 μM
    Compound: Calcitriol
    Antipoliferative activity against human HepG2 cells after 48 hrs by MTT assay
    Antipoliferative activity against human HepG2 cells after 48 hrs by MTT assay
    [PMID: 26562542]
    HL-60 EC50
    0.009 μM
    Compound: Calcitriol
    Agonist activity at vitamin D3 receptor in human HL-60 cells assessed as induction of cell differentiation after 96 hrs by NBT dye-based microscopic analysis
    Agonist activity at vitamin D3 receptor in human HL-60 cells assessed as induction of cell differentiation after 96 hrs by NBT dye-based microscopic analysis
    [PMID: 26562542]
    HL-60 IC50
    0.05 μM
    Compound: 1, 1,25(OH)2D3, calcitriol
    Induction of cell differentiation of human HL60 cells incubated for 144 hrs by Wst-1 dye based assay
    Induction of cell differentiation of human HL60 cells incubated for 144 hrs by Wst-1 dye based assay
    [PMID: 25180926]
    HL-60 EC50
    17.9 nM
    Compound: Calcitriol
    Induction of human HL60 cell differentiation after 4 days by NBT reduction assay
    Induction of human HL60 cell differentiation after 4 days by NBT reduction assay
    [PMID: 24035340]
    HL-60 ED50
    2 nM
    Compound: 1, calcitriol, 1alpha,25-(OH)2D3
    Induction of differentiation of human HL60 promyelocytes to monocytes after 4 days by nitro blue tetrazolium reduction assay
    Induction of differentiation of human HL60 promyelocytes to monocytes after 4 days by nitro blue tetrazolium reduction assay
    [PMID: 26206427]
    HL-60 ED50
    2 nM
    Compound: 1, calcitriol, 1alpha,25-(OH)2D3
    Induction of human HL60 cell differentiation after 4 days by NBT reduction assay
    Induction of human HL60 cell differentiation after 4 days by NBT reduction assay
    [PMID: 22490010]
    HL-60 EC50
    2 nM
    Compound: 1, 1alpha,25-(OH)2D3, calcitriol
    Induction of differentiation of human HL60 promyelocytes into monocytes after 4 days by NBT reduction assay
    Induction of differentiation of human HL60 promyelocytes into monocytes after 4 days by NBT reduction assay
    [PMID: 19819702]
    HL-60 EC50
    2 nM
    Compound: 1, 1alpha,25(OH)2D3, calcitriol
    Induction of differentiation of human HL-60 cells promyelocytes to monocytes after 4 days by NBT reduction assay
    Induction of differentiation of human HL-60 cells promyelocytes to monocytes after 4 days by NBT reduction assay
    [PMID: 18722130]
    HL-60 EC50
    2 nM
    Compound: 1, calcitriol
    Induction of differention of human HL60 cells into monocytes by NBT reduction assay
    Induction of differention of human HL60 cells into monocytes by NBT reduction assay
    [PMID: 17960924]
    HL-60 EC50
    2150 pM
    Compound: 1, 1,25-(OH)2D3
    Induction of human HL60 cell differentiation to monocytes by NBT reduction assay
    Induction of human HL60 cell differentiation to monocytes by NBT reduction assay
    [PMID: 17298045]
    HL-60 EC50
    3 nM
    Compound: 1, Calcitriol, 1alpha,25-(OH)2D3
    Induction of human HL60 cell differentiation after 4 days by nitro blue tetrazolium reduction assay
    Induction of human HL60 cell differentiation after 4 days by nitro blue tetrazolium reduction assay
    [PMID: 22018918]
    HL-60 ED50
    3 nM
    Compound: 1; calcitriol; 1alpha,25-(OH)2D3
    Induction of human HL60 cell differentiation assessed as differentiation from promyelocytes to monocytes by NBT assay
    Induction of human HL60 cell differentiation assessed as differentiation from promyelocytes to monocytes by NBT assay
    [PMID: 26630444]
    HL-60 ED50
    3 nM
    Compound: 1, 1alpha,25-(OH)2D3,calcitriol
    Induction of human HL60 cell differentiation into monocytes after 4 days by NBT reduction assay
    Induction of human HL60 cell differentiation into monocytes after 4 days by NBT reduction assay
    [PMID: 19402630]
    HL-60 EC50
    3 nM
    Compound: 1, calcitriol
    Induction of cell differentiation of human HL60 cells to monocytes by NBT reduction assay
    Induction of cell differentiation of human HL60 cells to monocytes by NBT reduction assay
    [PMID: 19167893]
    HN12 IC50
    4.68 nM
    Compound: 1b, calcitriol
    Cytotoxicity against human HN12 assessed as decrease in cell count after 120 hrs
    Cytotoxicity against human HN12 assessed as decrease in cell count after 120 hrs
    [PMID: 22926068]
    HN12 IC50
    553 nM
    Compound: calcitriol
    Antiproliferative activity against human HN12 cells assessed as decrease in cell number after 72 hrs by WST assay
    Antiproliferative activity against human HN12 cells assessed as decrease in cell number after 72 hrs by WST assay
    [PMID: 24900339]
    HOS EC50
    0.01 nM
    Compound: 1alpha,25(OH)2D3
    Activity at human VDR expressed in human HOS cells transfected with pGL3-hOc, pCDNA-hVDR and phRL-TK assessed as assessed as transcriptional activation measured 24 hrs post infection by luciferase reporter gene assay
    Activity at human VDR expressed in human HOS cells transfected with pGL3-hOc, pCDNA-hVDR and phRL-TK assessed as assessed as transcriptional activation measured 24 hrs post infection by luciferase reporter gene assay
    [PMID: 21889334]
    HOS EC50
    0.011 nM
    Compound: 1-alpha,25(OH)2D3
    Agonist activity at human VDR expressed in HOS cells co-expressing human RXR by Dual-Glo luciferase reporter gene assay
    Agonist activity at human VDR expressed in HOS cells co-expressing human RXR by Dual-Glo luciferase reporter gene assay
    [PMID: 30446437]
    Huh-7 EC50
    0.0003 μM
    Compound: 1alpha,25-dihydroxyvitamin D3
    Agonist activity at VDR expressed in human HuH7 cells after 24 hrs by pDR3-luciferase reporter gene assay
    Agonist activity at VDR expressed in human HuH7 cells after 24 hrs by pDR3-luciferase reporter gene assay
    [PMID: 27145071]
    Jurkat EC50
    3.936 nM
    Compound: 1,25(OH)2D3
    Activation of VDR in human Jurkat cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay
    Activation of VDR in human Jurkat cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay
    [PMID: 27070779]
    L02 IC50
    0.67 μM
    Compound: Calcitriol
    Antiproliferative activity against human L02 cells after 48 hrs by MTT assay
    Antiproliferative activity against human L02 cells after 48 hrs by MTT assay
    [PMID: 29518319]
    L02 IC50
    0.67 μM
    Compound: Calcitriol
    Cytotoxicity against human L02 cells after 48 hrs by MTT assay
    Cytotoxicity against human L02 cells after 48 hrs by MTT assay
    [PMID: 26562542]
    L02 IC50
    48 μM
    Compound: 1; 1,25(OH)2D3
    Cytotoxicity against human LO2 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    Cytotoxicity against human LO2 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    [PMID: 30579121]
    MCF7 IC50
    > 50 μM
    Compound: 3; 1,25(OH)2D3
    Antiproliferative activity against human MCF7 cells expressing VDR siRNA assessed as reduction in BrdU incorporation after 16 hrs by ELISA
    Antiproliferative activity against human MCF7 cells expressing VDR siRNA assessed as reduction in BrdU incorporation after 16 hrs by ELISA
    [PMID: 30193216]
    MCF7 IC50
    11.1 μM
    Compound: 1; 1,25(OH)2D3
    Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay
    [PMID: 30579121]
    MCF7 IC50
    11.43 μM
    Compound: 3; 1,25(OH)2D3
    Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay
    [PMID: 30193216]
    MCF7 IC50
    12.5 μM
    Compound: 1alpha,25-dihydroxyvitamin D3
    Antiproliferative activity against human MCF7 cells assessed as inhibition of proliferation after 72 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells assessed as inhibition of proliferation after 72 hrs by MTT assay
    [PMID: 25127149]
    MCF7 EC50
    3.28 nM
    Compound: 1, 1alpha,25-(OH)2D3, 1,25D, calcitriol
    Agonist activity at VDR in human MCF7 cells assessed as transcription of CYP24A1 gene after 24 hrs by luciferase reporter gene assay
    Agonist activity at VDR in human MCF7 cells assessed as transcription of CYP24A1 gene after 24 hrs by luciferase reporter gene assay
    [PMID: 22989379]
    MCF7 EC50
    5.2 x 10-2 μM
    Compound: 1
    Antiproliferative activity against human MCF7 cells after 72 hrs by [3H]thymidine incorporation assay
    Antiproliferative activity against human MCF7 cells after 72 hrs by [3H]thymidine incorporation assay
    [PMID: 19739672]
    MCF7 EC50
    5.5 nM
    Compound: 1alpha,25(OH)2D3
    Agonist activity at zebrafish gal4-VDR LBD expressed in human MCF7 cells by luciferase reporter gene based transactivation assay
    Agonist activity at zebrafish gal4-VDR LBD expressed in human MCF7 cells by luciferase reporter gene based transactivation assay
    [PMID: 22180837]
    MCF7 IC50
    5.59 μM
    Compound: Calcitriol
    Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
    [PMID: 29518319]
    MCF7 IC50
    5.6 μM
    Compound: Calcitriol
    Antipoliferative activity against human MCF7 cells after 48 hrs by MTT assay
    Antipoliferative activity against human MCF7 cells after 48 hrs by MTT assay
    [PMID: 26562542]
    Medulloblastoma cell GI50
    1.4 μM
    Compound: 3
    Antiproliferative activity against medulloblastoma cells derived from conditional patched knockout mouse after 48 hrs by [3H]-thymidine incorporation assay
    Antiproliferative activity against medulloblastoma cells derived from conditional patched knockout mouse after 48 hrs by [3H]-thymidine incorporation assay
    [PMID: 30471551]
    PBMC IC50
    1 nM
    Compound: 1
    Inhibition of LPS-induced IL12/23p40 production in human PBMC after 24 hrs by ELISA
    Inhibition of LPS-induced IL12/23p40 production in human PBMC after 24 hrs by ELISA
    [PMID: 19309155]
    PBMC IC50
    1.2 x 10-2 μM
    Compound: 1
    Inhibition of LPS-induced IL6 production in human PBMC after 24 hrs by ELISA
    Inhibition of LPS-induced IL6 production in human PBMC after 24 hrs by ELISA
    [PMID: 19309155]
    PBMC IC50
    29 pM
    Compound: 1
    Inhibition of LPS-induced TNFalpha production in human PBMC after 24 hrs by ELISA
    Inhibition of LPS-induced TNFalpha production in human PBMC after 24 hrs by ELISA
    [PMID: 19309155]
    PBMC IC50
    8 nM
    Compound: 1
    Inhibition of IFN-gamma production in human PBMC after 5 days by ELISA-based mixed lymphocyte reaction assay
    Inhibition of IFN-gamma production in human PBMC after 5 days by ELISA-based mixed lymphocyte reaction assay
    [PMID: 19309155]
    PC-3 IC50
    17.2 μM
    Compound: Calcitriol
    Antipoliferative activity against human PC3 cells after 48 hrs by MTT assay
    Antipoliferative activity against human PC3 cells after 48 hrs by MTT assay
    [PMID: 26562542]
    PC-3 IC50
    17.25 μM
    Compound: Calcitriol
    Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay
    Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay
    [PMID: 29518319]
    PC-3 IC50
    9.53 μM
    Compound: 3; 1,25(OH)2D3
    Antiproliferative activity against human PC3 cells after 24 hrs by MTT assay
    Antiproliferative activity against human PC3 cells after 24 hrs by MTT assay
    [PMID: 30193216]
    SW480 IC50
    16.78 μM
    Compound: 78
    Anticancer activity against human SW480 cells assessed as reduction in cell proliferation incubated for 2 days by CCK-8 assay
    Anticancer activity against human SW480 cells assessed as reduction in cell proliferation incubated for 2 days by CCK-8 assay
    [PMID: 33445154]
    T47D IC50
    1.3 nM
    Compound: calcitriol
    Antiproliferative activity against human T47D cells assessed as decrease in cell number after 72 hrs by WST assay
    Antiproliferative activity against human T47D cells assessed as decrease in cell number after 72 hrs by WST assay
    [PMID: 24900339]
    THP-1 EC50
    1 x 10-2 μM
    Compound: 1
    Activation of VDR in human THP1 cells assessed as increase in 25-hydroxyvitamin D-24-hydroxylase mRNA expression by RT-PCR
    Activation of VDR in human THP1 cells assessed as increase in 25-hydroxyvitamin D-24-hydroxylase mRNA expression by RT-PCR
    [PMID: 19309155]
    THP-1 EC50
    1 x 10-2 μM
    Compound: 1
    Activation of VDR in human THP1 cells assessed as increase in cathelicidin antimicrobial peptide mRNA expression by RT-PCR
    Activation of VDR in human THP1 cells assessed as increase in cathelicidin antimicrobial peptide mRNA expression by RT-PCR
    [PMID: 19309155]
    体外研究
    (In Vitro)

    Calcitriol 对宫颈癌细胞具有体外抗增殖作用。与对照组相比,用 100 nM Calcitriol 处理 6 天后,细胞数量减少了 12.8%。随着 Calcitriol 浓度的增加,细胞增殖的抑制作用更加明显。200 nM 和 500 nM Calcitriol 分别减少了 26.1% 和 31.6%。用 Calcitriol 处理 72 小时后,G1 期细胞明显聚集,200 nM 约 66.18%,500 nM 约 78.10%,而对照组则为(24.36%)。与对照组相比,则为 治疗可显著降低 HCCR-1 蛋白表达,且呈时间和剂量依赖性[1]。 Calcitriol 可显著增加 ERα mRNA,且呈剂量依赖性,EC50 为 9.8×10-9 M[2]

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

    体内研究
    (In Vivo)

    长期使用 Calcitriol 处理(每天 150 ng/kg,持续 4.5 个月)可改善松弛(骨化三醇治疗的 OVX 大鼠中 pD2:6.30,Emax:68.6%)。OVX 大鼠双肾的肾血流量均减少,Calcitriol 可恢复血流量。长期使用 Calcitriol 可降低 OVX 大鼠肾动脉中 COX-2 和血栓素-前列腺素 (TP) 受体表达的增加[3]。高剂量和低剂量 Calcitriol 治疗使第 56 天的果糖喂养大鼠的收缩压 (SBP) 分别显著降低 14 和 9 mmHg。与其他组相比,高剂量 Calcitriol 治疗(每天 20 ng/kg)显著提高血清离子钙水平[4]

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

    Clinical Trial
    分子量

    416.64

    Formula

    C27H44O3

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    骨化三醇;钙三醇

    结构分类
    初始来源
    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    -20°C, protect from light, stored under nitrogen

    *该产品在溶液状态不稳定,建议您现用现配,即刻使用。

    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : 110 mg/mL (264.02 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 : 100 mg/mL (240.02 mM; 超声助溶)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.4002 mL 12.0009 mL 24.0017 mL
    5 mM 0.4800 mL 2.4002 mL 4.8003 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;该产品在溶液状态不稳定,建议您现用现配,即刻使用。

    • 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: 2.75 mg/mL (6.60 mM); 悬浊液; 超声助溶

      此方案可获得 2.75 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      1 mL 工作液为例,取 100 μL 27.5 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: ≥ 2.75 mg/mL (6.60 mM); 澄清溶液

      此方案可获得 ≥ 2.75 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 27.5 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。
    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)。

    *该产品在溶液状态不稳定,建议您现用现配,即刻使用。

    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: 99.94%

    参考文献
    Cell Assay
    [1]

    HeLa S3 cells are plated at a density of 1,000 cells/well in 96-well plates of Dulbecco’s modified Eagle’s medium (DMEM) with 10% fetal bovine serum (FBS), treated with 1% ethanol (control) or various concentrations of Calcitriol (100, 200, and 500 nM) for 72 h. A Cell Counting Kit8 (CCK-8) is used to determine cell proliferation. At 24, 48, 72, 96, 120, and 144 h after culturing with 200 nM Calcitriol, cells are harvested for analysis. Three independent experiments are performed in quadruplicate[1].

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

    Animal Administration
    [3]

    Adult female Sprague-Dawley rats weighing 200 to 220g are used in this study. Rats are housed in a temperature-controlled room (~23°C) with a 12-h light/dark cycle. The animals have free access to a standard diet and water. Ovariectomy (OVX) is performed on rats. At 6 months after the surgical procedure, the OVX rats are randomly assigned to either treatment with vehicle dimethyl sulfoxide (OVX+vehicle) or Calcitriol (150 ng/kg daily, OVX+calcitriol). Calcitriol treatment is given by oral gavage and lasted or 4.5 months. Blood pressure and serum Calcitriol level are measured[3].

    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;该产品在溶液状态不稳定,建议您现用现配,即刻使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    Ethanol / DMSO 1 mM 2.4002 mL 12.0009 mL 24.0017 mL 60.0043 mL
    5 mM 0.4800 mL 2.4002 mL 4.8003 mL 12.0009 mL
    10 mM 0.2400 mL 1.2001 mL 2.4002 mL 6.0004 mL
    15 mM 0.1600 mL 0.8001 mL 1.6001 mL 4.0003 mL
    20 mM 0.1200 mL 0.6000 mL 1.2001 mL 3.0002 mL
    25 mM 0.0960 mL 0.4800 mL 0.9601 mL 2.4002 mL
    30 mM 0.0800 mL 0.4000 mL 0.8001 mL 2.0001 mL
    40 mM 0.0600 mL 0.3000 mL 0.6000 mL 1.5001 mL
    50 mM 0.0480 mL 0.2400 mL 0.4800 mL 1.2001 mL
    60 mM 0.0400 mL 0.2000 mL 0.4000 mL 1.0001 mL
    80 mM 0.0300 mL 0.1500 mL 0.3000 mL 0.7501 mL
    100 mM 0.0240 mL 0.1200 mL 0.2400 mL 0.6000 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.

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    产品名称:
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