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Epelsiban(GSK 557296)
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(GSK 557296)图片
CAS NO:872599-83-2

Epelsiban (GSK 557296) (GSK 557296) 是一种有效的、选择性的和口服生物可利用的催产素受体拮抗剂，对人催产素受体的 pKi 为 9.9。
Cas No.872599-83-2
别名GSK 557296
Canonical SMILESO=C(N1CCOCC1)[C@@H](C2=C(N=C(C)C=C2)C)N3[C@](C(N[C@H](C4CC5=CC=CC=C5C4)C3=O)=O)([H])[C@@H](C)CC
分子式C30H38N4O4
分子量518.65
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Epelsiban (GSK 557296) is a potent, selective and orally bioavailable oxytocin receptor antagonist, with a pKi of 9.9 for human oxytocin receptor.

Epelsiban 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,

Epelsiban shows an IC50 of 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].

[1]. Borthwick AD, et al. Pyridyl-2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists: synthesis, pharmacokinetics, and in vivo potency. J Med Chem. 2012 Jan 26;55(2):783-96.

 
 
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