[CAS NO. 834153-87-6] (R)-Elagolix

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PRODUCTS SPECIFICATIONS [834153-87-6]

Catalog

HY-14789

Brand

MCE

CAS

834153-87-6

DESCRIPTION [834153-87-6]

Overview

MDL	-
Molecular Weight	631.59
Molecular Formula	C32H30F5N3O5
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

For research use only. We do not sell to patients.

Summary

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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT04445025	Colorado Center for Reproductive Medicine\|AbbVie	Infertility\|Endometriosis	September 1, 2020	Early Phase 1
NCT04333576	AbbVie	Endometriosis	August 10, 2020	Phase 3
NCT00109512	Abbott	Endometriosis	April 2005	Phase 2
NCT03746535	Yale University	Endometriosis	July 1, 2022	Early Phase 1
NCT04856306	Medstar Health Research Institute	Heavy Menstrual Bleeding\|Fibroid Uterus	April 12, 2021
NCT03271489	AbbVie	Heavy Menstrual Bleeding\|Uterine Fibroids	September 13, 2017	Phase 3
NCT03343067	AbbVie	Endometriosis	December 27, 2017	Phase 3
NCT02691494	AbbVie	Uterine Fibroids\|Heavy Menstrual Bleeding	February 3, 2016	Phase 3
NCT02925494	AbbVie	Uterine Fibroids\|Heavy Menstrual Bleeding	September 14, 2016	Phase 3
NCT04060992	University of Southern California	Ovulation; Failure or Lack of	October 1, 2019	Phase 4
NCT04039204	Wake Forest University Health Sciences\|University of North Carolina, Chapel Hill\|Stanford University	Endometriosis\|Unexplained Infertility	January 15, 2022	Phase 2
NCT00619866	AbbVie	Endometriosis, Pain	February 19, 2008	Phase 2
NCT01441635	AbbVie (prior sponsor, Abbott)\|AbbVie	Heavy Uterine Bleeding\|Uterine Fibroids	September 8, 2011	Phase 2
NCT01760954	AbbVie	Endometriosis	December 28, 2012	Phase 3
NCT01817530	AbbVie	Heavy Uterine Bleeding\|Uterine Fibroids	April 8, 2013	Phase 2
NCT03951077	AbbVie	Polycystic Ovary Syndrome	August 12, 2019	Phase 2
NCT00973973	AbbVie	Endometriosis, Pain	October 12, 2009	Phase 2
NCT01620528	AbbVie (prior sponsor, Abbott)\|AbbVie	Endometriosis	May 22, 2012	Phase 3
NCT00437658	AbbVie	Endometriosis	December 11, 2006	Phase 2
NCT04614246	Bayer	Endometriosis	January 29, 2021	Phase 2
NCT03886220	AbbVie	Uterine Fibroids	April 12, 2019	Phase 4
NCT02654054	AbbVie	Uterine Fibroids\|Heavy Menstrual Bleeding	December 22, 2015	Phase 3
NCT04173169	Yale University\|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)\|University of Colorado, Denver\|Northwestern University\|University of North Carolina	Infertility\|Endometriosis	March 15, 2022	Phase 3
NCT00797225	AbbVie	Endometriosis	November 26, 2008	Phase 2
NCT03213457	AbbVie	Endometriosis	July 7, 2017	Phase 3
NCT01403038	AbbVie (prior sponsor, Abbott)\|Neurocrine Biosciences\|AbbVie	Folliculogenesis	June 2011	Phase 1
NCT02143713	AbbVie	Endometriosis	May 27, 2014	Phase 3
NCT01931670	AbbVie	Endometriosis	September 9, 2013	Phase 3
NCT05038878	Icahn School of Medicine at Mount Sinai\|AbbVie	Mild Autonomous Cortisol Excess	July 6, 2021	Phase 4

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL ( 158.33 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.5833 mL	7.9165 mL	15.8331 mL
5 mM	0.3167 mL	1.5833 mL	3.1666 mL
10 mM	0.1583 mL	0.7917 mL	1.5833 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (3.96 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (3.96 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (3.96 mM); Clear solution

* All of the co-solvents are available by MCE.

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.

Synonyms

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]-

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]butanoic acid

NBI 56418

Elagolix

(R)-4-((2-(5-(2-Fluoro-3-methoxyphenyl)-3-(2-fluoro-6-(trifluoromethyl)benzyl)-4-methyl-2,6-dioxo-2,3-dihydropyrimidin-1(6H)-yl)-1-phenylethyl)amino)butanoic acid