L-368,899
L-368,899 is an orally active and selective OT (oxytocin) receptor antagonist, with IC50s of 8.9 and 26 nM for uterus of rat and human, respectively. L-368,899 can cross the blood-brain barrier (BBB) . L-368,899 inhibits oxytocin-stimulated uterine contractions in rats and can be used in study of preterm labor[1][2][3].
Product Specifications
CAS Number
148927-60-0
UNSPSC
12352005
Target
Oxytocin Receptor
Type
Reference compound
Related Pathways
GPCR/G Protein
Applications
Metabolism-protein/nucleotide metabolism
Field of Research
Endocrinology
Assay Protocol
https://www.medchemexpress.com/l-368-899.html
Solubility
10 mM in DMSO
Smiles
O=S(C[C@]12[C@H](C[C@@H](CC2)C1(C)C)NC([C@@H](N)CCS(C)(=O)=O)=O)(N3CCN(C4=C(C=CC=C4)C)CC3)=O
Molecular Formula
C26H42N4O5S2
Molecular Weight
554.77
References & Citations
[1]Pettibone D J, et al. L‐368,899, a potent orally active oxytocin antagonist for potential use in preterm labor[J]. Drug development research, 1993, 30 (3) : 129-142. |[2]Mann GE, et al. Attenuation of PGF2alpha release in ewes infused with the oxytocin antagonist L-368,899. Domest Anim Endocrinol. 2003 Oct;25 (3) :255-62.|[3]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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
Phase 1
Citation 01
J Headache Pain. 2025 Aug 6;26 (1) :179.|Mater Technol (N Y N Y) . 2025 Jun 17.|bioRxiv. 2024 May 14.|Cell. 2025 Jun 26;188 (13) :3530-3549.e24.|Front Pharmacol. 2019 Nov 15;10:1380.|Neurosci Res. 2021 Jul:168:41-53.
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