Formulation: A crystalline solid
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
Purity: ≥98%
Formula Markup: C32H29F5N3O5 • Na
Formula Weight: 653,6
Shelf life (days): 1460
CAS Number: 832720-36-2
Notes: Elagolix is an antagonist of the gonadotropin-releasing hormone receptor (GnRHR; Ki = 0.9 nM in a radioligand binding assay).{45161} It is selective for GnRHR over the cytochrome P450 (CYP) isoform CYP3A4 (IC50 = 56 μM) as well as a panel of 100 receptors, ion channels, enzymes, and transporters (IC50s = >10 μM). Elagolix inhibits GnRH-induced inositol phosphate production in RBL-1 cells expressing human GnRHR (IC50 = 1.5 nM). In vivo, elagolix (30 mg/kg) suppresses production of luteinizing hormone in castrated male cynomolgus macaques. Formulations containing elagolix have been used in the treatment of endometriosis.
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