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(R) -Elagolix

CAT: 0804-HY-14789-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-14789-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
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].
CAS Number
834153-87-6
Product Name Alternative
NBI-56418
UNSPSC
12352005
Hazard Statement
H315, H319, H335
Target
GnRH Receptor; Nuclear Factor of activated T Cells (NFAT)
Type
Reference compound
Related Pathways
GPCR/G Protein; Immunology/Inflammation
Applications
Cancer-programmed cell death
Field of Research
Cancer; Endocrinology
Assay Protocol
https://www.medchemexpress.com/Elagolix.html
Concentration
10mM
Purity
96.05
Solubility
DMSO : 62.5 mg/mL (ultrasonic; warming; heat to 60°C)
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
Molecular Formula
C32H30F5N3O5
Molecular Weight
631.59
Precautions
H315, H319, H335
References & Citations
[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.|[2]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|[3]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.|[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.|[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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Launched

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