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Epelsiban

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Company Name: Fan De(Beijing) Biotechnology Co., Ltd.  
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Email: liming@bio-fount.com
Company Name: Shanghai zhigan biotechnology co., LTD  
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Company Name: BOC Sciences  
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Company Name: TargetMol Chemicals Inc.  
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Company Name: TargetMol Chemicals Inc.  
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Epelsiban manufacturers

  • Epelsiban
  • Epelsiban pictures
  • $3700.00
  • 2026-05-11
  • CAS:872599-83-2
  • Purity:
  • Supply Ability: 10g
  • Epelsiban
  • Epelsiban pictures
  • $3700.00
  • 2025-07-18
  • CAS:872599-83-2
  • Purity:
  • Supply Ability: 10g
Epelsiban Basic information
Product Name:Epelsiban
Synonyms:Epelsiban;(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;GSK 557296;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)-;(3R,6R)-6-((S)-sec-butyl)-3-(2,3-dihydro-1H-inden-2-yl)-1-((R)-1-(2,6-dimethylpyridin-3-yl)-2-morpholino-2-oxoethyl)piperazine-2,5-dione
CAS:872599-83-2
MF:C30H38N4O4
MW:518.65
EINECS:
Product Categories:
Mol File:872599-83-2.mol
Epelsiban Structure
Epelsiban 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
pka13.16±0.60(Predicted)
Safety Information
MSDS Information
Epelsiban Usage And Synthesis
UsesEpelsiban (GSK 557296) is a potent, selective and orally bioavailable oxytocin receptor antagonist, with a pKi of 9.9 for human oxytocin receptor.
DefinitionChEBI: 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
Epelsiban Preparation Products And Raw materials
Tag:Epelsiban(872599-83-2) Related Product Information
Epelsiban Oxytocin PF-06655075 Retosiban (S)-2-(4-methyl-1,4-diazepane-1-carbonothioyl)-N-(2-methyl-4-(1-methyl-1,4,5,10-tetrahydrobenzo[b]pyrazolo[3,4-e][1,4]diazepine-5-carbonyl)benzyl)pyrrolidine-1-carboxamide Biotin-CYIQNCPLG-NH2 (disulfide bridge: 1-6)