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Epelsiban

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Epelsiban
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Cat #: V3618 CAS #: 872599-83-2 Purity ≥ 98%

Description: Epelsiban (also known as GSK557296; GSK-557296) is a novel, potent, selective and orally bioavailable oxytocin receptor antagonist, with a pKi of 9.9 for human oxytocin receptor. It was initially developed by GSK for the treatment of premature ejaculation in men and then as an agent to enhance embryo or blastocyst implantation in women undergoing embryo or blastocyst transfer associated with in vitro fertilization. Later it was also investigated for use in the treatment of adenomyosis. Epelsiban shows >31000-fold selectivity over all three human vasopressin receptors hV1aR, hV2R, and hV1bR, with no significant P450 inhibition. Epelsiban has low levels of intrinsic clearance against the microsomes of four species, good bioavailability (55%) and comparable potency to atosiban in the rat, but is 100-fold more potent than the latter in vitro and was negative in the genotoxicity screens with a satisfactory oral safety profile in female rats.

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CAS No.872599-83-2
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
ProtocolIn VitroEpelsiban (GSK557296; GSK-557296) 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 VivoEpelsiban 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].
These protocols are for reference only. InvivoChem does not independently validate these methods.
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