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Epelsiban

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Catalog No. T11502Cas No. 872599-83-2
Alias GSK 557296

Epelsiban is a selective and orally bioavailable oxytocin receptor antagonist (pKi: 9.9 for human oxytocin receptor).

Epelsiban

Epelsiban

😃Good
Catalog No. T11502Alias GSK 557296Cas No. 872599-83-2
Epelsiban is a selective and orally bioavailable oxytocin receptor antagonist (pKi: 9.9 for human oxytocin receptor).
Pack SizePriceAvailabilityQuantity
25 mg$2,1208-10 weeks
50 mg$2,7808-10 weeks
100 mg$3,7008-10 weeks
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Product Introduction

Bioactivity
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.
AliasGSK 557296
Chemical Properties
Molecular Weight518.65
FormulaC30H38N4O4
Cas No.872599-83-2
Relative Density.1.214 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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