NBI42902

Cas No.:	352290-60-9
Chemical Name:	3-[(2R)-Amino-2-phenylethyl]-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)-6-methylpyrimidin-2,4-dione
Synonyms:	NBI-42902,NBI 42902
SMILES:	O=C1N(C[C@H](N)C2=CC=CC=C2)C(C(C3=CC=CC(OC)=C3F)=C(C)N1CC4=C(F)C=CC=C4F)=O
Formula:	C27H24F3N3O3
M.Wt:	495.49
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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.For the detailed information of NBI42902, the solubility of NBI42902 in water, the solubility of NBI42902 in DMSO, the solubility of NBI42902 in PBS buffer, the animal experiment (test) of NBI42902, the cell expriment (test) of NBI42902, the in vivo, in vitro and clinical trial test of NBI42902, the EC50, IC50,and Affinity of NBI42902, Please contact DC Chemicals.