Shopping Cart
- Remove All
- Your shopping cart is currently empty
Epelsiban is a selective and orally bioavailable oxytocin receptor antagonist (pKi: 9.9 for human oxytocin receptor).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $2,120 | 8-10 weeks | |
50 mg | $2,780 | 8-10 weeks | |
100 mg | $3,700 | 8-10 weeks |
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. |
Alias | GSK 557296 |
Molecular Weight | 518.65 |
Formula | C30H38N4O4 |
Cas No. | 872599-83-2 |
Relative Density. | 1.214 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Copyright © 2015-2024 TargetMol Chemicals Inc. All Rights Reserved.