T 98475 is a novel, potent and orally active nonpeptide antagonist of the LHRH receptor.
ChEBI: 7-[(2,6-difluorophenyl)methyl]-2-[4-[(2-methyl-1-oxopropyl)amino]phenyl]-3-[[methyl-(phenylmethyl)amino]methyl]-4-oxo-5-thieno[2,3-b]pyridinecarboxylic acid propan-2-yl ester is a thienopyridine and an isopropyl ester.
Potent, orally active and non-peptide gonadotropin-releasing hormone (GnRH, LHRH) receptor antagonist (IC 50 values are 0.2, 4.0 and 60 nM for human, monkey and rat GnRH receptors respectively). Inhibits LH release in vitro (IC 50 = 100 nM) and reduces plasma LH concentration in castrated male cynomolgus monkeys.
