NBI-42902 - CAS 352290-60-9

NBI-42902 is a potent inhibitor of peptide radioligand binding to the human GnRH receptor (K (i) = 0.56 nm) . Tritiated NBI-42902 binds with high affinity (K (d) = 0.19 nm) to a single class of binding sites and can be displaced by a range of peptide and nonpeptide GnRH receptor ligands. In vitro experiments demonstrate that NBI-42902 is a potent functional, competitive antagonist of GnRH stimulated IP accumulation, Ca (2+) flux, and ERK1/2 activation. It did not stimulate histamine release from rat peritoneal mast cells. Finally, it is effective in lowering serum LH in castrated male macaques after oral administration. Overall, these data provide a benchmark of pharmacological characteristics required for a nonpeptide GnRH antagonist to effectively suppress gonadotropins in humans and suggest that NBI-42902 may have clinical utility as an oral agent for suppression of the hypothalamic-pituitary-gonadal axis. (source: Endocrinology. 2007 Feb;148 (2) :857-67. Epub 2006 Nov 9.)

Others, PERK, GNRH Receptor

Others, GPCR/G Protein, Apoptosis

352221

C27H24F3N3O3

495.49

CC1=C(C(=O)N(C[C@H](N)C2=CC=CC=C2)C(=O)N1CC3=C(F)C=CC=C3F)C4=C(F)C(OC)=CC=C4

-20°C

Ice Packs

Small Compound