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

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

Epelsiban is a potent oxytocin receptor, with a pK_iof 9.9 for human oxytocin receptor, >31000-fold selectivity over all three human vasopressin receptors hV1aR (pK_i,<5.2), hV2R (pK_i,<5.1), and hV1bR (pK_i, 5.4), and shows no significant P450 inhibition^[1].

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].

518.65

C₃₀H₃₈N₄O₄

872599-83-2

Room temperature in continental US; may vary elsewhere.

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