Catalog Number: 2641
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.
Background References
  1. Attenuation of PGE release in ewes infused with the oxytocin antagonist L-368,899.
    Mann et al.
    Domest.Anim.Endocrinol., 2003;25:255
  2. Oral oxytocin antagonists.
    Borthwick
    J.Med.Chem., 2010;53:6525
  3. Discovery and development of a new class of potent, selective, orally active oxytocin receptor antagonist.
    Quattropani et al.
    J.Med.Chem., 2005;48:7882
  4. 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 util
    Williams et al.
    J.Med.Chem., 1994;37:565
Citations:

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

2 Citations: Showing 1 - 2
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  1. Oxytocin-stimulated NFAT transcriptional activation in human myometrial cells.
    Authors: Pont Et al.
    Mol.Endocrinol. 2012;26:1743
  2. The fat-induced satiety factor oleoylethanolamide suppresses feeding through central release of oxytocin.
    Authors: Gaetani Et al.
    Nat Commun 2010;30:8096

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