Epelsiban

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Epelsiban
File:Epelsiban structure.svg
Systematic (IUPAC) name
(3R,6R)-3-(2,3-dihydro-1H-inden-2-yl)-1-[(1R)-1-(2,6-dimethylpyridin-3-yl)-2-(morpholin-4-yl)-2-oxoethyl]-6-[(1S)-1-methylpropyl]piperazine-2,5-dione
Clinical data
Legal status
  • Non-regulated
Identifiers
CAS Number 872599-83-2
1159097-48-9 (besylate)
ATC code None
PubChem CID: 11634973
ChemSpider 9809717
KEGG D10117 YesY
Chemical data
Formula C30H38N4O4
Molecular mass 518.6 g/mol
  • CC[C@H](C)[C@@H]1C(=O)N[C@@H](C(=O)N1[C@H](C2=C(N=C(C=C2)C)C)C(=O)N3CCOCC3)C4CC5=CC=CC=C5C4
  • InChI=1S/C30H38N4O4/c1-5-18(2)26-28(35)32-25(23-16-21-8-6-7-9-22(21)17-23)29(36)34(26)27(24-11-10-19(3)31-20(24)4)30(37)33-12-14-38-15-13-33/h6-11,18,23,25-27H,5,12-17H2,1-4H3,(H,32,35)/t18-,25+,26+,27+/m0/s1
  • Key:UWHCWRQFNKUYCG-QUZACWSFSA-N

Epelsiban (GSK-557,296-B)[1][2] is an oral drug which acts as a selective, sub-nanomolar (Ki=0.13 nM) oxytocin receptor antagonist with >31000-fold selectivity over the related vasopressin receptors and is being developed by GlaxoSmithKline for the treatment of premature ejaculation in men.[3][4] and as an agent to enhance embryo or blastocyst implantation in women undergoing embryo or blastocyst transfer associated with in vitro fertilization (IVF).[5]

See also

References

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