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Calcitriol

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Chemical Structure| 32222-06-3 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 : 416.637
MDL号 : MFCD00867079
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(252.02 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 100 mg/mL(240.02 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
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].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 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

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

[1]24(9):876-887.

[2]74(4):1451-1455.

[3]Shang M, Sun J. Vitamin D/VDR, Probiotics, and Gastrointestinal Diseases. Curr Med Chem. 2017;24(9):876-887.