147657-22-5
147657-22-5 結(jié)構(gòu)式
基本信息
卡泊三醇單水合物
卡泊三醇一水合物
鈣泊三醇一水合物 EP標(biāo)準(zhǔn)品
卡泊三醇一水合物, 鈣泊三醇一水合物
Calcipotriol monohydrate CRS
Calcipotriol (Calcipotriene) Monohydrate
(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 hydrate
(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)-
物理化學(xué)性質(zhì)
常見問題列表
鈣泊三醇是維生素D類物質(zhì)，鈣泊三醇以兩種晶態(tài)形式無水物和一水合物。鈣泊三醇一水合物的藥效學(xué)性質(zhì)與維生素D3活性代謝產(chǎn)物骨化三醇相似，但不易引起高鈣血癥。
鈣泊三醇[CAS112965-21-6]在抑制不期望的表皮角質(zhì)化細胞增殖方面展示很強的活性。已在許多臨床試驗中證實了卡泊三醇和鈣泊三醇一水合物在治療牛皮癬方面的功效，且目前在許多商業(yè)藥物制劑中均使用鈣泊三醇。
vitamin D receptor
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.
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).