AG-045572

A GnRH receptor antagonist (Kis = 6, 2.2, and 3.8 nM for the human, mouse, and rat receptors, respectively), selective for the GnRH receptor over a panel of 43 receptors, ion channels, and enzymes at 1 µM, prevents GnRH-induced increases in inositol phosphate production in HEK293 cells expressing the human GnRH receptor (KB = 25 nM), oral or intravenous administration decreases plasma LH levels in castrated rats, inhibits GnRH-A-induced increases in plasma LH and testosterone levels in non-castrated rats at 20 mg/kg. Formulation: A solid. InChI: InChI=1S/C30H37NO5/c1-18-13-22-23(30(4,5)12-11-29(22,2)3)15-19(18)14-20-9-10-24(36-20)28(32)31-27-25(34-7)16-21(33-6)17-26(27)35-8/h9-10,13,15-17H,11-12,14H2,1-8H3,(H,31,32). InChIKey: IPEMCIBPDYCJLO-UHFFFAOYSA-N. SMILES: CC1(CCC(C)(C2=CC(C)=C(CC3=CC=C(C(NC4=C(OC)C=C(OC)C=C4OC)=O)O3)C=C12)C)C