Calcipotriol monohydrate 是维生素 D3 的类似物,对维生素 D 受体具有高亲和力。Calcipotriol monohydrate 可用于银屑病研究。
产品描述
Calcipotriol monohydrate is an analog of Vitamin D3 with a high affinity for the vitamin D receptor. Calcipotriol monohydrate can be used for studies about psoriasis.
体外活性
Calcipotriol monohydrate (100, 10, and 1 ng/mL) significantly upregulated the expression of NKp30 on the surface of NK cells after 4 h incubation[1]. When NHEK cells are not stimulated with IL-17A or IL-22, Calcipotriol monohydrate 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 monohydrate (2, 20 and 40 nM) in a dose dependent manner[2].
体内活性
The weight gain is significantly smaller in the groups treated with Diclofenac plus Calcipotriol monohydrate (p=0.018) and Diclofenac plus DFMO plus Calcipotriol monohydrate (p=0.002) compare with placebo (linear regression model)[3].
细胞实验
Normal human epidermal keratinocytes are grown in serum-free keratinocyte growth medium Epilife and used at the third passage in all experiments. The growth supplement is omitted 48 h before experiments. As a control, IL-17A and IL-22 are either added or not added to the cells. Cultured NHEK cells are stimulated with IL-17A (200 ng/mL) and/or IL-22 (200 ng/mL) followed by co-incubation in the presence or absence of Calcipotriol at 0.2-40 nM to test its modulatory effect. Cells are harvested 3 days later and subjected to real-time qPCR. Culture supernatants are also collected and frozen at -80°C until used for ELISA [1].
动物实验
The 160 female SKH-1 hairless mice (6-7 weeks of age) are used. After UV treatment, mice without tumors are randomly divided into five groups, four chemoprevention groups (Diclofenac plus DFMO; Diclofenac plus Calcipotriol; DFMO plus calcitriol; and Diclofenac plus DFMO plus Calcipotriol) and one placebo group (skin lotion). The mice are treated with test mixtures once a day, five days a week, for a total of 17 weeks. The test mixtures are applied topically on the dorsal surface of the mice. Ten microliters are applied by a pipette after which the mixture is rubbed onto the skin. This corresponded to the following doses of each active substance in the treatments: 100 μg/week for Diclofenac (30 mg/g undiluted), 0.166 μg/week for Calcitriol (50 μg/g undiluted), and 463.3 μg/week for DFMO (139 mg/g undiluted) [3].
Cas No.
147657-22-5
分子式
C27H42O4
分子量
430.62
别名
钙泊三醇一水合物;卡泊三醇一水合物;Calcipotriol monohydrate
储存和溶解度
DMSO:95 mg/mL (220.61 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years