卡泊三醇一水合物 TQ0244

Product Introduction
Bioactivity


英文名: Calcipotriol monohydrate

描述: 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。

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].

体外活性: Calcipotriol monohydrate（100, 10, 和 1 ng/mL）显著提升了NK细胞表面NKp30的表达量，在4小时的孵育后[1]。当NHEK细胞未被IL-17A或IL-22刺激时，Calcipotriol monohydrate轻微增强（0.2 nM）IL-8 mRNA表达，或无影响（2-20 nM）。加入IL-17A和IL-22后，IL-8的mRNA表达显著提升，证实了我们之前的研究。这种IL-8 mRNA表达的增强，通过Calcipotriol monohydrate（2, 20 和 40 nM）以剂量依赖方式被抑制[2]。

体内活性: 在经过Diclofenac加Calcipotriol monohydrate（p=0.018）和Diclofenac加DFMO加Calcipotriol monohydrate（p=0.002）处理的组别中，与安慰剂（线性回归模型）[3]相比，体重增加显著较小。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 95 mg/mL (220.61 mM)
DMSO : 95 mg/mL (220.61 mM)


关键字: VD/VDR | Vitamin D receptor | Calcipotriol | Vitamin D | Calcipotriol monohydrate | Calcipotriol Monohydrate | inhibit | Inhibitor

相关库: Drug Repurposing Compound Library | Approved Drug Library | Bioactive Compounds Library Max | EMA Approved Drug Library | Metabolism Compound Library | Bioactive Compound Library

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