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Epelsiban
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Epelsiban图片
CAS NO:872599-83-2
包装:5 mg
市场价:7000元

产品名称
GSK 557296
产品介绍

产品描述

Epelsiban is a selective and orally bioavailable oxytocin receptor antagonist (pKi: 9.9 for human oxytocin receptor).

体外活性

Epelsiban , shows no significant P450 inhibition.?is a potent oxytocin receptor, with a pKi of 9.9 for human oxytocin receptor, >31000-fold selectivity over all three human vasopressin receptors hV1aR (pKi,<5.2), hV2R (pKi,<5.1), and hV1bR (pKi, 5.4).

体内活性

Epelsiban has low levels of intrinsic clearance against the microsomes of rat, dog, and cynomolgus monkey, good bioavailability (55%), but is negative in the genotoxicity screens with a satisfactory oral safety profile in female rats.Epelsiban shows an IC50 of 192 nM for oxytocin receptor in rats.

Cas No.

872599-83-2

分子式

C30H38N4O4

分子量

518.65

别名

GSK 557296

储存和溶解度

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years