2455524-81-7
Chemical Structure
Elagolix-d9
- CAS No.: 2455524-81-7
- Formula:C32H21D9F5N3O5
- Molecular Weight:640.65
InChIKey: HEAUOKZIVMZVQL-OJJUFRRJSA-N
SMILES: CC1=C(C2=C(C(OC([2H])([2H])[2H])=CC=C2)F)C(N(C(N1CC3=C(C=CC=C3F)C(F)(F)F)=O)C[C@@H](C4=CC=CC=C4)NC([2H])([2H])C([2H])([2H])C([2H])([2H])C(O)=O)=O
Biological Activity: Elagolix-d9 is the deuterium labeled Elagolix. 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].
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Elagolix-d9 | Elagolix-d9 is the deuterium labeled Elagolix. 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. . | |||||||||||||||||||||
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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. | |||||||||||||||||||||
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- [1]. 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
- [2]. 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]
- [3]. 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]
- [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. [Content Brief]
- [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. [Content Brief]
Keywords
