Epelsiban

Name: Epelsiban
Brand: TargetMol
SKU: T11502
Rating: 4.5 (1 reviews)

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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

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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 Size	Price	Availability
25 mg	$2,120	8-10 weeks
50 mg	$2,780	8-10 weeks
100 mg	$3,700	8-10 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):192 nM , OTR (human):(pKi)9.9
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

Chemical Properties

Molecular Weight	518.65
Formula	C₃₀H₃₈N₄O₄
Cas No.	872599-83-2
Relative Density.	1.214 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | 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 DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

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