Elagolix

Elagolix is an orally active, highly effective, selective and non-peptide gonadotropin-releasing hormone receptor (GnRH receptor) antagonist (KD = 54 pM) and NFAT inhibitor, which can be used to study pain related to endometriosis[1][2][3][4][5].

Product Specifications

CAS Number

[2323071-30-1]

UNSPSC

12352005

Target

GnRH Receptor; Nuclear Factor of activated T Cells (NFAT)

Related Pathways

GPCR/G Protein; Immunology/Inflammation

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Cancer; Metabolic Disease

Smiles

O=C(O)CCCNC(C1=CC=CC=C1)CN(C(N(CC2=C(C(F)(F)F)C=CC=C2F)C(C)=C3C4=CC=CC(OC)=C4F)=O)C3=O

Molecular Formula

C32H30F5N3O5

Molecular Weight

631.59

References & Citations

[1]Kim SM, et al. Discovery of an Orally Bioavailable Gonadotropin-Releasing Hormone Receptor Antagonist. J Med Chem. 2016 Oct 13;59 (19) :9150-9172. Epub 2016 Sep 27.|[2]Chen C, et al. Discovery of sodium R- (+) -4-{2-[5- (2-fluoro-3-methoxyphenyl) -3- (2-fluoro-6-[trifluoromethyl]benzyl) -4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human gonadotropin-releasing hormone receptor. J Med Chem. 2008 Dec 11;51 (23) :7478-85.|[3]Qiong Wang, et al. Analytical methodology and pharmacokinetic study of elagolix in plasma of rats using a newly developed UPLC-MS/MS assay. Arabian Journal of Chemistry. Volume 14, Issue 7, July 2021, 103235|[4]Mohammad Ezzati, et al. Elagolix, a novel, orally bioavailable GnRH antagonist under investigation for the treatment of endometriosis-related pain. Womens Health (Lond) . 2015 Jan;11 (1) :19-28.|[5]Carr B, et al. Elagolix, an oral GnRH antagonist, versus subcutaneous depot medroxyprogesterone acetate for the treatment of endometriosis: effects on bone mineral density. Reprod Sci. 2014 Nov;21 (11) :1341-1351.