L-368,899 hydrochloride

Cat. No. 2641

L-368,899 hydrochloride C26H42N4O5S2.HCl [160312-62-9]

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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 V1a 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 -20°C
CAS No:
160312-62-9

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

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

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.

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

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.

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Citations are publications that use Tocris products. Selected citations for L-368,899 hydrochloride include:

Pont et al (2012) Oxytocin-stimulated NFAT transcriptional activation in human myometrial cells. Mol.Endocrinol. 26 1743. PMID: 22902539.

Gaetani et al (2010) The fat-induced satiety factor oleoylethanolamide suppresses feeding through central release of oxytocin. Nat Commun 30 8096. PMID: 20554860.

Do you know of a great paper that uses L-368,899 hydrochloride from Tocris? If so please let us know.

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Keywords: L-368,899 hydrochloride, supplier, Potent, non-peptide, oxytocin, receptor, antagonists, OT, Receptors, L368899, Tocris Bioscience, Oxytocin Receptor Antagonist products

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