1. GPCR/G Protein
  2. Oxytocin Receptor
  3. Epelsiban

Epelsiban (Synonyms: GSK 557296)

Cat. No.: HY-105018
Handling Instructions

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

For research use only. We do not sell to patients.

Epelsiban Chemical Structure

Epelsiban Chemical Structure

CAS No. : 872599-83-2

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Description

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

IC50 & Target

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

In Vitro

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].

Clinical Trial
Molecular Weight

518.65

Formula

C₃₀H₃₈N₄O₄

CAS No.

872599-83-2

SMILES

O=C(N1CCOCC1)[[email protected]@H](C2=C(N=C(C)C=C2)C)N3[[email protected]](C(N[[email protected]](C4CC5=CC=CC=C5C4)C3=O)=O)([H])[[email protected]@H](C)CC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

EpelsibanGSK 557296GSK557296GSK-557296Oxytocin ReceptorOXTRInhibitorinhibitorinhibit

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