834153-87-6
Chemical Structure
(R)-Elagolix
Synonym(s): NBI-56418
- CAS No.: 834153-87-6
- Formula:C32H30F5N3O5
- Molecular Weight:631.59
IUPAC Name: (R)-4-((2-(5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-(trifluoromethyl)benzyl)-4-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)-1-phenylethyl)amino)butanoic acid
InChIKey: HEAUOKZIVMZVQL-VWLOTQADSA-N
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
Biological Activity: 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].
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(R)-Elagolix | 96.05% | 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. . | ||||||||||||||||||||
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(R)-Elagolix (Standard) | ≥98% | (R)-Elagolix (Standard) is the analytical standard of (R)-Elagolix. This product is intended for research and analytical applications. 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. . | ||||||||||||||||||||
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References
- [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. [Content Brief]
- [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. [Content Brief]
- [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. [Content Brief]
- [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. [Content Brief]
