285571-64-4

285571-64-4 structure

Name: barusiban
Chemical Name: (4S,7S,10S,16R)-N-[(2S)-5-amino-1-hydroxypentan-2-yl]-7-(2-amino-2-oxoethyl)-13-[(2S)-butan-2-yl]-10-[(2R)-butan-2-yl]-16-(1H-indol-3-ylmethyl)-N-methyl-6,9,12,15,18-pentaoxo-1-thia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
CAS Number: 285571-64-4
Molecular Formula: C₄₀H₆₃N₉O₈S
Molecular Weight: 830.04900
Catalog: Signaling Pathways GPCR/G Protein Oxytocin Receptor
Create Date: 2016-11-02 18:44:38
Modify Date: 2024-01-03 14:22:14
Barusiban (FE-200440) is an oxytocin receptor (OT-R) antagonist (Ki=0.8 nM), inhibits OT-induced contraction. Barusiban can be used in preterm labor (PTL), in vitro fertilisation (IVF) and infertility research[1][2][3].

Name	(4S,7S,10S,16R)-N-[(2S)-5-amino-1-hydroxypentan-2-yl]-7-(2-amino-2-oxoethyl)-13-[(2S)-butan-2-yl]-10-[(2R)-butan-2-yl]-16-(1H-indol-3-ylmethyl)-N-methyl-6,9,12,15,18-pentaoxo-1-thia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
Synonyms	FE200 440 Barusiban [INN] UNII-UX33I93GLS Barusiban C4.6,S1-Cyclo(N-(3-sulfanylpropanoyl)-D-tryptophyl-L-isoleucyl-L-alloisoleucyl-L-asparaginyl-L-2-aminobutanoyl-N-methyl-L-ornithinol)

Description	Barusiban (FE-200440) is an oxytocin receptor (OT-R) antagonist (Ki=0.8 nM), inhibits OT-induced contraction. Barusiban can be used in preterm labor (PTL), in vitro fertilisation (IVF) and infertility research[1][2][3].
Related Catalog	Research Areas >> Endocrinology Signaling Pathways >> GPCR/G Protein >> Oxytocin Receptor
In Vitro	Barusiban shows affinity for oxytocin receptor (Ki=0.8 nM) in COS cells expressed with oxytocin receptor[3].
In Vivo	Barusiban (intravenous injection; 50 or 150 μg/kg; once) treatment shows inhibition on OT-induced contractions[2]. Animal Model: Pregnant cynomolgus monkeys injected with oxytocin (OT)[2] Dosage: 50 or 150 μg/kg Administration: Intravenous injection; 50 or 150 μg/kg; once Result: Reduced uterine contractions to baseline levels effectively. Reduced intrauterine pressure (IUP) from 6-7.5 kmm Hg•h to approximately 1 kmm Hg•h.