Description
An antagonist of GnRHR (Ki = 0.9 nM in a radioligand binding assay); selective for GnRHR over CYP3A4 (IC50 = 56 μM) as well as a panel of 100 receptors, ion channels, enzymes, and transporters (IC50s = >10 μM); inhibits GnRH-induced inositol phosphate production in RBL-1 cells expressing human GnRHR (IC50 = 1.5 nM); suppresses production of luteinizing hormone in castrated male cynomolgus macaques at 30 mg/kg
Formal name: 4-[[(1R)-2-[5-(2-fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-3,6-dihydro-4-methyl-2,6-dioxo-1(2H)-pyrimidinyl]-1-phenylethyl]amino]-butanoic acid, monosodium salt
Synonyms:
Molecular weight: 653.6
CAS: 832720-36-2
Purity: ≥98%
Formulation: A crystalline solid
Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Endocrinology & Metabolism|Hormones & Receptors||Research Area|Endocrinology & Metabolism|Reproductive Biology
