Epelsiban

Name: Epelsiban
Brand: TargetMol
SKU: T11502
Price: 171 USD
Availability: InStock
Rating: 4.5 (1 reviews)

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产品编号 T11502Cas号 872599-83-2

别名 GSK 557296

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

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产品编号 T11502 别名 GSK 557296Cas号 872599-83-2

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

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产品介绍

生物活性

产品描述	Epelsiban is a selective and orally bioavailable oxytocin receptor antagonist (pKi: 9.9 for human oxytocin receptor).
靶点活性	OTR (human):(pKi)9.9 , OTR (human):192 nM
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.
别名	GSK 557296