Epelsiban_product_DataBase

Bioactivity	Epelsiban (GSK 557296) is a potent, selective and orally bioavailable oxytocin receptor antagonist, with a pKi of 9.9 for human oxytocin receptor.
Target	pKi: 9.9 (human oxytocin receptor)IC50: 192 nM (human oxytocin receptor)
Invitro	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, <5.2), hV2R (pKi, <5.1), and hV1bR (pKi, 5.4), and shows no significant P450 inhibition[1].
In Vivo	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].
Name	Epelsiban
CAS	872599-83-2
Formula	C30H38N4O4
Molar Mass	518.65
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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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