| 生物活性： |
靶点：VD/VDR
通路：Others
背景说明：Calcitriol是一种非选择性vitamin D receptor的激活剂。
生物活性：Calcitriol is the most active metabolite of vitamin D and also a vitamin D receptor (VDR) agonist.[1-4]
In Vitro：Calcitriol exerts antiproliferative effects on cervical cancer cells in vitro. Cells decrease by 12.8% when treated with 100 nM Calcitriol for 6 days， compare with control. Inhibition of cell proliferation becomes more pronounced with the increase in Calcitriol concentration. The decrease is 26.1% and 31.6% for 200 and 500 nM Calcitriol， respectively. Treatment with Calcitriol for 72 h induces an evident accumulation of cells in the G1 phase， with approximately 66.18% in 200 nM and 78.10% in 500 nM， compare with the control (24.36%). Calcitriol treatment significantly decreases HCCR-1 protein expression compare with the control in a time- and dose-dependent manner[1]. Calcitriol significantly increases ERα mRNA in a dose dependent manner with an EC50 of 9.8×10-9 M[2].
In Vivo：Chronic treatment with Calcitriol (150 ng/kg per day for 4.5 months) improves the relaxations (pD2: 6.30±0.09， Emax: 68.6±3.9% in Calcitriol-treated OVX， n=8). Renal blood flow in OVX rats is reduced in both kidneys， and the flow is restored by Calcitriol treatment. The increased expression of COX-2 and Thromboxane-prostanoid (TP) receptor in OVX rat renal arteries is reduced by chronic calcitriol administration[3]. High- and low-dose Calcitriol treatment significantly decreases the systolic blood pressure (SBP) in the fructose-fed rats by 14±4 and 9±4 mmHg， respectively， at Day 56. High-dose Calcitriol treatment (20 ng/kg per day) significantly increases serum ionized calcium level (1.44±0.05 mmol/L) compare with the other groups[4].
细胞实验：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].
动物实验：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].
数据来源文献：[1]. Wang G， et al. Calcitriol Inhibits Cervical Cancer Cell Proliferation Through Downregulation of HCCR1 Expression. Oncol Res. 2014;22(5-6):301-9.
[2]. Santos-Martínez N， et al. Calcitriol restores antiestrogen responsiveness in estrogen receptor negative breast cancer cells: a potential new therapeutic approach. BMC Cancer. 2014 Mar 29;14:230.
[3]. Dong J， et al. Calcitriol restores renovascular function in estrogen-deficient rats through downregulation of cyclooxygenase-2 and the thromboxane-prostanoid receptor. Kidney Int. 2013 Jul;84(1):54-63.
[4]. Chou CL， et al. Beneficial effects of calcitriol on hypertension， glucose intolerance， impairment of endothelium-dependent vascular relaxation， and visceral adiposity in fructose-fed hypertensive rats. PLoS One. 2015 Mar 16;10(3):e0119843.
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| 其它标识： |
MDL：MFCD00867079
SMILES：CC(CCCC(C)(C)O)C1CCC2C1(CCCC2=CC=C3CC(CC(C3=C)O)O)C
InChIKey：GMRQFYUYWCNGIN-NKMMMXOESA-N
InChI：InChI=1S/C27H44O3/c1-18(8-6-14-26(3，4)30)23-12-13-24-20(9-7-15-27(23，24)5)10-11-21-16-22(28)17-25(29)19(21)2/h10-11，18，22-25，28-30H，2，6-9，12-17H2，1，3-5H3/b20-10+，21-11-/t18-，22-，23-，24+，25+，27-/m1/s1
PubChem CID：5280453
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| 基本信息： |
CAS：32222-06-3
中文名称：骨化三醇
英文名称：Calcitriol
别名：RO215535;Topitriol;Rocaltrol;Calcijex;25-Dihydroxyvitamin D3
分子式：C27H44O3
分子量：416.64
规格：5mg
溶解性：Soluble in DMSO/Ethanol ≥10mg/mL(该产品在溶液状态不稳定，建议您现用现配)
纯度：HPLC≥98%
外观(性状)：White to off-white Solid
储存条件：Powder:-20℃，2 years
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| 靶点： |
VD/VDR |
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