160312-62-9

160312-62-9 structure

Name: L-368,899 hydrochloride
Chemical Name: L-368,899 hydrochloride
CAS Number: 160312-62-9
Molecular Formula: C₂₆H₄₃ClN₄O₅S₂
Molecular Weight: 591.226
Catalog: Signaling Pathways GPCR/G Protein Oxytocin Receptor
Create Date: 2018-09-05 00:41:43
Modify Date: 2024-01-11 19:03:55
L-368,899 hydrochloride is a potent, selective, orally bioavailable, non-peptide oxytocin receptor antagonist, with IC50s of 8.9 nM and 26 nM for rat uterus and human uterus oxytocin receptor, respectively, used as a tocolytic agent.

Name	L-368,899 hydrochloride
Synonyms	(2S)-2-Amino-N-[(2S)-7,7-dimethyl-1-({[4-(2-methylphenyl)piperazin-1-yl]sulfonyl}methyl)bicyclo[2.2.1]hept-2-yl]-4-(methylsulfonyl)butanamide hydrochloride (1:1) Butanamide, 2-amino-N-[(2S)-7,7-dimethyl-1-[[[4-(2-methylphenyl)-1-piperazinyl]sulfonyl]methyl]bicyclo[2.2.1]hept-2-yl]-4-(methylsulfonyl)-, (2S)-, hydrochloride (1:1) (2S)-2-Amino-N-[(2S)-7,7-dimethyl-1-({[4-(2-methylphenyl)-1-piperazinyl]sulfonyl}methyl)bicyclo[2.2.1]hept-2-yl]-4-(methylsulfonyl)butanamide hydrochloride (1:1)

Description	L-368,899 hydrochloride is a potent, selective, orally bioavailable, non-peptide oxytocin receptor antagonist, with IC50s of 8.9 nM and 26 nM for rat uterus and human uterus oxytocin receptor, respectively, used as a tocolytic agent.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Oxytocin Receptor Research Areas >> Others
Target	IC50: 8.9 nM (rat uterus oxytocin receptor), 26 nM (human uterus oxytocin receptor)[1]
In Vitro	L-368,899 hydrochloride is a potent, orally bioavailable, non-peptide oxytocin receptor antagonist, with IC50s of 8.9 nM and 26 nM for rat uterus and human uterus oxytocin receptor, respectively. L-368,899 is less active on vasopressin receptor in human liver and kidney, rat liver and kidney (IC50, 510 nM, 960 nM, 890 nM, 2400 nM, respectively)[1].
References	[1]. Williams PD, et al. 1-((7,7-Dimethyl-2(S)-(2(S)-amino-4-(methylsulfonyl)butyramido)bicyclo [2.2.1]-heptan-1(S)-yl)methyl)sulfonyl)-4-(2-methylphenyl)piperaz ine (L-368,899): an orally bioavailable, non-peptide oxytocin antagonist with potential utility for managing preterm labor. J Med Chem. 1994 Mar 4;37(5):565-71.