An antagonist of GnRHR
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Elagolix (sodium salt)

Item No. 26534

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
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, monosodium salt
CAS Number
832720-36-2
Molecular Formula
C32H29F5N3O5 • Na
Formula Weight
653.6
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 12.5 mg/mlDMSO: 10 mg/mlEthanol: 10 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
275 nm
SMILES
O=C(N(CC1=C(F)C=CC=C1C(F)(F)F)C(C)=C2C3=C(F)C(OC)=CC=C3)N(C[C@H](NCCCC([O-])=O)C4=CC=CC=C4)C2=O.[Na+]
InChi Code
InChI=1S/C32H30F5N3O5.Na/c1-19-28(21-11-6-14-26(45-2)29(21)34)30(43)40(18-25(20-9-4-3-5-10-20)38-16-8-15-27(41)42)31(44)39(19)17-22-23(32(35,36)37)12-7-13-24(22)33;/h3-7,9-14,25,38H,8,15-18H2,1-2H3,(H,41,42);/q;+1/p-1/t25-;/m0./s1
InChi Key
DQYGXRQUFSRDCH-UQIIZPHYSA-M
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $90

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    10 mg

    $158

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    25 mg

    $349

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    Product Description

    Elagolix is an antagonist of the gonadotropin-releasing hormone receptor (GnRHR; Ki = 0.9 nM in a radioligand binding assay).1 It is selective for GnRHR over the cytochrome P450 (CYP) isoform CYP3A4 (IC50 = 56 μM) as well as a panel of 100 receptors, ion channels, enzymes, and transporters (IC50s = >10 μM). Elagolix inhibits GnRH-induced inositol phosphate production in RBL-1 cells expressing human GnRHR (IC50 = 1.5 nM). In vivo, elagolix (30 mg/kg) suppresses production of luteinizing hormone in castrated male cynomolgus macaques. Formulations containing elagolix have been used in the treatment of endometriosis.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Chen, D., Wu, D., Guo, Z., 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. 51(23), 7478-7485 (2008).