NBI-42902 |
| Catalog No.GC70777 |
NBI-42902 est un antagoniste des récepteurs de la GnRH actif par voie orale, puissant et fonctionnel, avec des valeurs de CI50 de 0,79 nm et 0,56 nm, respectivement.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 352290-60-9
Sample solution is provided at 25 µL, 10mM.
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NBI-42902 (0-1000 nM) is quite sensitive to the relatively conservative sequence changes between species, with IC50 values of 0.79 nM (human), 10 nM (macaque), 400 nM (dog), 200 nM (rabbit) for the GnRH receptors[1].
NBI-42902 (1 nM-1 μM, 1 min) inhibits GnRH (4 nM)-stimulated Ca2+ flux in RBL cells with a mean IC50 value of 3.6 nM[1].
NBI-42902 (1 nM-1 μM, 1 min) inhibits GnRH (4 nM)-induced IP accumulation competitively in RBL cells[1].
NBI-42902 (1 nM-1 μM, 5 min) blocks GnRH-stimulated ERK1/2 phosphorylation completely in CHO-GnRHR cells with an IC50 value of 5.22 nM[1].
NBI-42902 (10-100 mg/kg, p.o. or i.v. ) inhibits serum LH levels significantly in castrated macaques[1].
References:
[1]. Struthers RS, et al. Pharmacological characterization of a novel nonpeptide antagonist of the human gonadotropin-releasing hormone receptor, NBI-42902. Endocrinology. 2007 Feb;148(2):857-67.
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