(R)-Elagolix

(R)-Elagolix

• CAS Number: 834153-87-6
• UNSPSC Description: Elagolix 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-programmed cell death
• Field of Research: Cancer; Endocrinology
• Assay Protocol: https://www.medchemexpress.com/Elagolix.html
• Solubility: DMSO : 62.5 mg/mL (ultrasonic;warming;heat to 60°C)
• Smiles: FC1=C(C2=C(C)N(CC3=C(C(F)(F)F)C=CC=C3F)C(N(C[C@](C4=CC=CC=C4)([H])NCCCC(O)=O)C2=O)=O)C=CC=C1OC
• Molecular Weight: 631.59
• References & Citations: [1]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.|[2]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|[3]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.|[4]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.|[5]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.
• Shipping Conditions: Room Temperature
• Clinical Information: Launched