Cas No.: | 834153-87-6 |
Chemical 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 |
Synonyms: | NBI56418 Na; NBI-56418; NBI 56418; ABT-620; ABT 620; ABT620; Elagolix. Orilissa |
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 |
Formula: | C32H30F5N3O5 |
M.Wt: | 631.6 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | Elagolix is a highly potent, selective, orally-active, short-duration, non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (KD = 54 pM). |
Target: | GnRH |
In Vitro: | Elagolix is a short-acting, nonpeptide, GnRH antagonist, administered orally, that unlike injectable depot GnRH agonists and antagonists, produces a dose-dependent suppression of ovarian estrogen production, that is, from partial suppression at lower doses to full suppression at higher doses. Elagolix is regarded as the frontrunner of a new class of GnRH inhibitors that have been denoted as second-generation, due to their non-peptide nature and oral bioavailability. |
References: | [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. |