872599-83-2

Name	Epelsiban
CAS	872599-83-2
Molecular Formula	C30H38N4O4
MDL Number	MFCD26961099
Molecular Weight	518.65
MOL File	872599-83-2.mol

Synonyms

Epelsiban GSK 557296 (3R,6R)-6-[(2S)-butan-2-yl]-3-(2,3-dihydro-1H-inden-2-yl)-1-[(1R)-1-(2,6-dimethylpyridin-3-yl)-2-morpholin-4-yl-2-oxoethyl]piperazine-2,5-dione 2,5-Piperazinedione, 3-(2,3-dihydro-1H-inden-2-yl)-1-[(1R)-1-(2,6-dimethyl-3-pyridinyl)-2-(4-morpholinyl)-2-oxoethyl]-6-[(1S)-1-methylpropyl]-, (3R,6R)-

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Chemical Properties

Boiling point	790.6±60.0 °C(Predicted)
density	1.214±0.06 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	Soluble in DMSO
pka	13.16±0.60(Predicted)

Hazard Information

Uses

Epelsiban (GSK 557296) is a potent, selective and orally bioavailable oxytocin receptor antagonist, with a pKi of 9.9 for human oxytocin receptor.

Definition

ChEBI: Epelsiban is a dipeptide.

in vivo

Epelsiban 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].

References

[1] Borthwick AD, et al. Pyridyl-2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists: synthesis, pharmacokinetics, and in vivo potency. J Med Chem. 2012 Jan 26;55(2):783-96. DOI:10.1021/jm201287w

Supplier

Fan De(Beijing) Biotechnology Co., Ltd.

Telephone 15911056312

Websitehttp://www.bio-fount.com/

Shanghai zhigan biotechnology co., LTD

Telephone

Websitehttps://www.chemicalbook.com/ShowSupplierProductsList31144/0_EN.htm

TargetMol Chemicals Inc.

Telephone 15002134094

Websitehttps://www.targetmol.cn/

Shandong Ziyi Pharmaceutical Co., Ltd.

Telephone 17860786593

Website

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