NBI-42902

Data Sheet For research use only. Not for human use.

Cat. No. ：BCP07260CAS No. ：352290-60-9Purity：98%

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CAS No.	352290-60-9	Cat. No.	BCP07260
Name	NBI-42902
Synonyms	NBI42902;NBI 42902;
SMILES
Chemical Name
Formula	C27H24F3N3O3	M. Wt	495.49
Purity	98%	Storage	Store at 4-8°C
Description	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.