Catalog Number: 2519
Chemical Name: 7-[(2,6-Difluorophenyl)methyl]-4,7-dihydro-2-[4-[(2-methyl-1-oxopropyl)amino]phenyl]-3-[[methyl(phenylmethyl)amino]methyl]-4-oxo-thieno[2,3-b]pyridine-5-carboxylic acid 1-methylethyl ester
Biological Activity
Potent, orally active and non-peptide gonadotropin-releasing hormone (GnRH, LHRH) receptor antagonist (IC50 values are 0.2, 4.0 and 60 nM for human, monkey and rat GnRH receptors respectively). Inhibits LH release in vitro (IC50 = 100 nM) and reduces plasma LH concentration in castrated male cynomolgus monkeys.
Technical Data
  • M.Wt:
    657.77
  • Formula:
    C37H37F2N3O4S
  • Solubility:
    Soluble to 50 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Desiccate at +4°C
  • CAS No:
    199119-18-1
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. Design, synthesis, and structure-activity relationships of thieno[2,3-b]pyridin-4-one derivatives as a novel class of potent, orally active, non-peptide luteinizing hormone-releasing hormone receptor antagonists.
    Imada et al.
    J.Med.Chem., 2006;49:3809
  2. Discovery of a novel, potent, and orally active nonpeptide antagonist of the human luteinizing hormone-releasing hormone (LHRH) receptor.
    Cho et al.
    J.Med.Chem., 1998;41:4190
  3. Discovery of a thieno[2,3-d]pyrimidine-2,4-dione bearing a p-methoxyureidophenyl moiety at the 6-position: a highly potent and orally bioavailable non-peptide antagonist for the human luteinizing hormone-releasing hormone receptor.
    Sasaki et al.
    J.Med.Chem., 2003;46:113

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