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

Elagolix (sodium salt) – 5 mg

Brand:
Cayman
CAS:
832720-36-2
Storage:
-20
UN-No:
Non-Hazardous - /

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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SKU: 26534 - 5 mg Category:

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

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