Elagolix sodium

• CAS Number:

  832720-36-2

• UNSPSC Description:

  Elagolix sodium is a highly effective, selective, oral-active, short-term, 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].

• Target Antigen:

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

• Type:

  Reference compound

• Related Pathways:

  GPCR/G Protein;Immunology/Inflammation

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Endocrinology; Cancer

• Assay Protocol:

  https://www.medchemexpress.com/Elagolix_sodium.html

• Solubility:

  DMSO : 50 mg/mL (ultrasonic)|H2O : ≥ 50 mg/mL

• Smiles:

  O=C(CCCN[C@@H](CN(C1=O)C(N(C(C)=C1C2=CC=CC(OC)=C2F)CC3=C(C=CC=C3F)C(F)(F)F)=O)C4=CC=CC=C4)O[Na]

• Molecular Weight:

  653.57

• 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.

• Shipping Conditions:

  Room Temperature

• Clinical Information:

  Launched