您好,欢迎来到试剂信息网! [登录] [免费注册]
试剂信息网
位置:首页 > 产品库 > Epelsiban
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
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
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
GSK 557296
产品介绍
Epelsiban (GSK 557296) 是一种有效的,选择性的,可口服的催产素受体 (oxytocin receptor) 抑制剂,对人催产素受体的pKi值为 9.9。
生物活性

Epelsiban (GSK 557296) is a potent, selective and orally bioavailableoxytocin receptorantagonist, with apKiof 9.9 for humanoxytocin receptor.

IC50& Target

pKi: 9.9 (human oxytocin receptor)[1]
IC50: 192 nM (human oxytocin receptor)[1]

体外研究
(In Vitro)

Epelsiban is a potent oxytocin receptor, with a pKiof 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), and shows no significant P450 inhibition[1].

体内研究
(In Vivo)

Epelsiban shows an IC50of 192 nM for oxytocin receptor in rats. 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[1].

Clinical Trial
分子量

518.65

Formula

C30H38N4O4

CAS 号

872599-83-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.