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 ActivityPotent, 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.
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For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Discovery of a novel, potent, and orally active nonpeptide antagonist of the human luteinizing hormone-releasing hormone (LHRH) receptor.
Cho et al.
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.
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.
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