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L-368,899 hydrochloride

Cat. No. 2641

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Chemical Name: (2S)-2-Amino-N-[(1S,2S,4R)-7,7-dimethyl-1-[[[4-(2-methylphenyl)-1-piperazinyl]sulfonyl]methyl]bicyclo[2.2.1]hept-2-yl]-4-(methylsulfonyl)butanamide

Biological Activity

Potent, non-peptide and orally active oxytocin receptor antagonist (IC₅₀ = 8.9 nM) that displays > 40-fold selectivity over vasopressin V_1a and V₂ receptors (IC₅₀ values are 370 and 570 nM respectively). Antagonizes oxytocin-induced uterine contractions in vitro and in vivo.

Technical Data

M.Wt:

591.23

Formula:

C₂₆H₄₂N₄O₅S₂.HCl

Solubility:

Soluble to 100 mM in water and to 100 mM in DMSO

Purity:

>97 %

Storage:

Store at +4°C

CAS No:

148927-60-0

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

References

Williams et al (1994) 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)piperazine (L-368,899): an orally bioavailable, non-peptide oxytocin antagonist with potential utility for managing preterm labor. J.Med.Chem. 37 565. PMID: 8126695.

Mann et al (2003) Attenuation of PGE_2α release in ewes infused with the oxytocin antagonist L-368,899. Domest.Anim.Endocrinol. 25 255. PMID: 14550509.

Quattropani et al (2005) Discovery and development of a new class of potent, selective, orally active oxytocin receptor antagonist. J.Med.Chem. 48 7882. PMID: 16302826.

Borthwick (2010) Oral oxytocin antagonists. J.Med.Chem. 53 6525. PMID: 20550119.

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Keywords: L-368,899 hydrochloride, supplier, Potent, non-peptide, oxytocin, receptor, antagonists, OT, Receptors, L368899

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7-TM Receptor Signaling

Written by T. Kenakin et al

'Seven Transmembrane Receptor Signaling' highlights the multiple behaviors of 7-TMs including G-protein-dependent and -independent signaling as well as the concept of collateral efficacy