化合物Relacorilant T16727

Product Introduction
Bioactivity


英文名: Relacorilant

描述: Relacorilant 是一种选择性和口服生物可利用的糖皮质激素受体拮抗剂（HepG2 TAT 试验中的 Kis 为 7.2 nM，在基于细胞的试验中对大鼠、人和猴糖皮质激素受体的 Kis 分别为 12、81.2、210 nM）。 它具有治疗库欣综合征的潜力。

体外活性: Relacorilant also displays effective inhibition on CYP2C8 and CYP3A4 (IC50s, 0.21, 1.3 μM, respectively). It also modestly inhibits CYP2C9, 2C19, 2D6, and 3A5 (ICC50s: 2, 8, 9, and 4.9 μM, respectively)[1].

体内活性: Relacorilant (30 mg/kg, p.o., twice a day) obviously blocks the effects on plasma insulin. It fully inhibits cortisone induced increase in plasma glucose in rats of exogenous Cushing’s syndrome, and a similar effect is also observed when administrated with of Relacorilant at 7.5 mg/kg twice a day [1].

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

溶解度: DMSO : 22.5 mg/mL (38.36 mM)


关键字: Relacorilant | CORT-125134 | CORT125134

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相关库: Drug Repurposing Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Clinical Compound Library | Bioactive Compounds Library Max | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | Orally Active Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途