Calcitriol
产品说明书
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同义名 : | 钙三醇 ;1,25-Dihydroxyvitamin D3; 1α,25-dihydroxy Vitamin D3; 1,25(OH)2D; 1α,25-(OH)2D3; 1,25-dihydroxycholecalciferol; Soltriol; Silkis; Topitriol; Calcijex; Rocaltrol |
| CAS号 : | 32222-06-3 | |
| 货号 : | A132740 | |
| 分子式 : | C27H44O3 | |
| 纯度 : | 99%+ | |
| 分子量 : | 416.64 | |
| MDL号 : | MFCD00867079 | |
| 存储条件： |
Pure form Inert atmosphere, store in freezer, under -20°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
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| 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]. | ||
| 细胞研究 | |||||
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| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活性说明 | 数据源 |
| COS1 cells | Function assay | Displacement of 1-alpha, 25-(OH)[3H]D3 from human VDR expressed in COS1 cells, IC50=0.8 nM | 17924616 | ||
| COS7 cells | Function assay | 24 h | Agonist activity at human VDR in COS7 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay, EC50=0.5 nM | 17904370 | |
| CV1 cells | Function assay | Activity on human VDR-mediated transcription of osteocalcin VDRE fused to thymidine kinase promoter/growth hormone reporter gene in CV1 cells, ED50=0.7 nM | 17149880 | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.40mL 0.48mL 0.24mL |
12.00mL 2.40mL 1.20mL |
24.00mL 4.80mL 2.40mL |
| 参考文献 |
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