Elagolix (sodium salt)

Elagolix (sodium salt)

CAT N°: 26534
Price:

122.00 103.70

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 ?M) as well as a panel of 100 receptors, ion channels, enzymes, and transporters (IC50s = >10 ?M). 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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