Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Epelsiban is a selective and orally bioavailable oxytocin receptor antagonist (pKi: 9.9 for human oxytocin receptor).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 8-10 weeks | $ 2,120.00 | |
50 mg | 8-10 weeks | $ 2,780.00 | |
100 mg | 8-10 weeks | $ 3,700.00 |
Description | Epelsiban is a selective and orally bioavailable oxytocin receptor antagonist (pKi: 9.9 for human oxytocin receptor). |
Targets&IC50 | OTR (human):(pKi)9.9 , OTR (human):192 nM |
In vitro | 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). |
In vivo | Epelsiban exhibits low intrinsic clearance in rat, dog, and cynomolgus monkey microsomes, demonstrating good bioavailability (55%) while showing no genotoxic effects, and maintaining a satisfactory safety profile when orally administered to female rats. Additionally, Epelsiban effectively inhibits the oxytocin receptor in rats with an IC50 of 192 nM. |
Synonyms | GSK 557296 |
Molecular Weight | 518.65 |
Formula | C30H38N4O4 |
CAS No. | 872599-83-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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Epelsiban 872599-83-2 Others GSK 557296 GSK-557296 GSK557296 inhibitor inhibit