卡泊三醇一水合物
中文名称:
卡泊三醇一水合物
中文同义词:
卡泊三醇一水合物;卡泊三醇单水合物;钙泊三醇一水合物;卡泊三醇一水合物, 钙泊三醇一水合物;钙泊三醇一水合物 EP标准品
英文名称:
CALCIPOTRIOL MONOHYDRATE
英文同义词:
CALCIPOTRIOL MONOHYDRATE;(1R,3S,5Z)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(1R,2E,4S)-4-cyclopropyl-4-hydroxy-1-methyl-2-buten-1-yl]octahydro-7a-methyl-4H-inden-4-ylidene]ethylidene]-4-methylene-1,3-Cyclohexanediol hydrate;(5Z,7E,22E,24S)-24-Cyclopropyl-9,10-secochola-5,7,10(19),22-tetraene-1α,3β,24-triol;(1R,3S,5Z)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(1R,2E,4S)-4-cyclopropyl-4-hydroxy-1-methyl-2-buten-1-yl]octahydro-7a-methyl-4H-inden-4-ylidene]ethylidene]-4-methylene-1,3-Cyclohexanediol monohydrate;1,3-Cyclohexanediol,5-[(2E)-2-[(1R,3aS,7aR)-1-[(1R,2E,4S)-4-cyclopropyl-4-hydroxy-1-methyl-2-buten-1-yl]octahydro-7a-methyl-4H-inden-4-ylidene]ethylidene]-4-methylene-,hydrate (1:1), (1R,3S,5Z)-;Calcipotriol (Calcipotriene) Monohydrate;Calcipotriol monohydrate CRS
CAS号:
147657-22-5
分子式:
C27H40O3.H2O
分子量:
430.625
EINECS号:
689-035-6
相关类别:
其它中间体;原料药;API;API intermediates
Mol文件:
147657-22-5.mol
溶解度
Practically insoluble in water, freely soluble in ethanol (96 per cent), slightly soluble in methylene chloride.
简介
钙泊三醇是维生素D类物质，钙泊三醇以两种晶态形式无水物和一水合物。钙泊三醇一水合物的药效学性质与维生素D3活性代谢产物骨化三醇相似，但不易引起高钙血症。
应用
钙泊三醇[CAS112965-21-6]在抑制不期望的表皮角质化细胞增殖方面展示很强的活性。已在许多临床试验中证实了卡泊三醇和钙泊三醇一水合物在治疗牛皮癣方面的功效，且目前在许多商业药物制剂中均使用钙泊三醇。
生物活性
Calcipotriol是1,25-Dihydroxyvitamin D3类似物，可作用于银屑病。
靶点
vitamin D receptor
体外研究
When NHEK cells are not stimulated with IL-17A or IL-22, Calcipotriol slightly enhances (0.2 nM) IL-8 mRNA expression or has no effect (2-20 nM). The addition of IL-17A and IL-22 markedly increased the mRNA expression of IL-8, confirming our previous study. This enhanced IL-8 mRNA expression is suppressed by Calcipotriol at 2, 20 and 40 nM in a dose dependent manner. Treatment of natural killer (NK) cells with drugs modulates their expression of NK cytotoxicity receptors or KIR. Human NK cells are pre-treated with 100, 10 or 1 ng/mL of 1,25(OH) 2 D 3 , Calcipotriol or FTY720 for 4 h. All three concentrations of 1,25(OH) 2 D 3 , Calcipotriol and FTY720 significantly up-regulate the expression of NKp30 on the surface of NK cells after 4 h incubation.
体内研究
One out of the 32 animals in each of the groups has died, except for the Diclofenac plus DFMO plus Calcipotriol group, where all animals survived. Survival is equally distributed between the groups. The weight gain is significantly smaller in the groups treated with Diclofenac plus Calcipotriol (p=0.018) and Diclofenac plus DFMO plus Calcipotriol (p=0.002) compare with placebo (linear regression model).
