L 366509 

L 366509 is a spiroindenylpiperidine camphorsulfonamide oxytocin (OT) antagonist. Modifications led to a new series of o-tolylpiperazine (TP) camphorsulfonamides, exhibiting high affinity for OT receptors and selectivity over arginine vasopressin receptors. Notably, compound 7 (L-368,899) showed excellent OT receptor affinity, potency in inhibiting OT-stimulated uterine contractions, good aqueous solubility, and oral bioavailability in multiple species. Compound 7 has entered clinical testing as an oral and intravenous tocolytic agent. Molecular modeling suggests the TP camphorsulfonamide structure mimics the D-AA2-Ile3 dipeptide, crucial in potent OT antagonists^[1].

459.60

C₂₅H₃₃NO₅S

138382-23-7

O=S(N(CC1)CCC21C3=CC=CC=C3C=C2)(C[C@]4(C5(C)C)CC[C@@H]5C[C@@]4(CC(O)=O)O)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. 1- (( (7,7-Dimet hyl-2( S)-(2( S)-amino-4- (met hylsulfonyl) butyramido) bicyclo[2.2.1]- heptan-l( S)-yl)methyl)sulfonyl)-4-(2-methylphenyl)piperazine (L-368,899): An Orally Bioavailable, Non-Peptide Oxytocin Antagonist with Potential Utility for Managing Preterm Labor