NBI-42902 |
| カタログ番号GC70777 |
NBI-42902は経口活性、強力な機能性、競合するGnRH受容体アンタゴニストであり、IC 50値はそれぞれ0.79 nMと0.56 nMである。
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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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