CAS:32222-06-3Calcitriol

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Synonyms: Ro-215535;Topitriol;1,25-Dihydroxyvitamin D3;Rocaltrol

Calcitriol is a vitamin D receptor agonist with IC50 of 0.4 nM.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

32222-06-3

储存条件

分子式

C27H44O3

运输

蓝冰

分子量

416.64

别名

Ro-215535;Topitriol;1,25-Dihydroxyvitamin D3;Rocaltrol

溶解度

DMSO	370.0 mg/mL (888.1 mM)
Water	insoluble

动物实验配方

生物活性

描述VDR (vitamin D receptor), as a member of the nuclear receptor superfamily, mediates the biological activity of 1,25-dihydroxyvitamin D3 (calcitriol) which is generated from vitamin D by successive hydroxylations in the liver and kidney. VDR can regulate a variety of illnesses in intestine, kidney, bone, skin, heart, and various other organs^[3]. Calcitriol, the most biologically active metabolite of vitamin D, is a non-selective VDR agonist with IC₅₀ of 0.4 nM. Calcitriol is a potent inhibitor of PHA (phytohemagglutinin)-induced lymphocyte proliferation, achieving 70% inhibition of tritiated thymidine incorporation after 72 h in culture. Furthermore, calcitriol suppresses interleukin-2 (IL-2) production by PHA-stimulated peripheral blood mononuclear cells in a concentration-dependent fashion^[4]. In HL-60 cells, a human myelomonocytic leukemia cell line, calcitriol arrests cells in G1; this effect is mediated through an increase in p27. Calcitriol mediated arrest in G0/G1 is also observed in human breastcancer lines. In vivo, a decrease in tumor volume induced by calcitriol correlates with a significant decrease in the intratumoral p21 expression^[5].