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elagolix

Names

[ CAS No. ]:
834153-87-6

[ Name ]:
elagolix

[Synonym ]:
4-[[(1R)-2-[5-(2-fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-4-methyl-2,6-dioxopyrimidin-1-yl]-1-phenylethyl]amino]butanoic acid
4-({(1R)-2-[5-(2-Fluoro-3-methoxyphenyl)-3-[2-fluoro-6-(trifluoromethyl)benzyl]-4-methyl-2,6-dioxo-3,6-dihydro-1(2H)-pyrimidinyl]-1-phenylethyl}amino)butanoic acid
Butanoic acid, 4-[[(1R)-2-[5-(2-fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-3,6-dihydro-4-methyl-2,6-dioxo-1(2H)-pyrimidinyl]-1-phenylethyl]amino]-
Elagolix

Biological Activity

[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: GnRHin 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.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> GNRH Receptor
Research Areas >> Cancer

[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.


[Related Small Molecules]

(Des-Gly10,D-Leu6,Pro-NHEt9)-LHRH acetate salt | Alarelin | Cetrorelix Acetate | [D-Trp6]-LH-RH | (D-Ser(tBu)6,AzaGly10)-LHRH acetate salt | Deslorelin | Buserelin (Acetate) | Relugolix | (D-2-Nal6)-LHRH acetate salt | Elagolix sodium | Gonadorelin Acetate | (Des-Gly10,tBu-D-Gly6,Pro-NHEt9)-LHRH trifluoroacetate salt | opigolix

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
728.6±70.0 °C at 760 mmHg

[ Molecular Formula ]:
C32H30F5N3O5

[ Molecular Weight ]:
631.590

[ Flash Point ]:
394.5±35.7 °C

[ Exact Mass ]:
631.210571

[ PSA ]:
102.56000

[ LogP ]:
7.20

[ Vapour Pressure ]:
0.0±2.5 mmHg at 25°C

[ Index of Refraction ]:
1.567

[ Storage condition ]:
2-8℃

Synthetic Route

Click to get detail synthetic route

Related Compounds