1. GPCR/G Protein
  2. GNRH Receptor
  3. Elagolix sodium

Elagolix sodium (Synonyms: NBI-56418 sodium)

Cat. No.: HY-14369 Purity: 99.20%
Handling Instructions

Elagolix sodium is a human GnRH receptor (GnRHR) antagonist with an IC50 and Ki of 0.25 and 3.7 nM, respectively.

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

Elagolix sodium Chemical Structure

Elagolix sodium Chemical Structure

CAS No. : 832720-36-2

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 101 In-stock
Estimated Time of Arrival: December 31
5 mg USD 70 In-stock
Estimated Time of Arrival: December 31
10 mg USD 110 In-stock
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 650 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Elagolix sodium is a human GnRH receptor (GnRHR) antagonist with an IC50 and Ki of 0.25 and 3.7 nM, respectively.

IC50 & Target

IC50: 0.25 nM (GnRHR)[1]
Ki: 3.7 nM (GnRHR)[2]

In Vitro

Elagolix sodium is a human GnRH receptor (GnRHR) antagonist with an IC50 of 0.25 nM in Kinase assay. Elagolix sodium has advanced to phase 3 trials for the treatment of endometriosis and uterine fibroids. Elagolix sodium also shows NFAT inhibition with an IC50 of 5.4 nM and effectively blocks Ca2+ flux with an IC50 of 0.86 nM[1]. Kinase assay also demonstrates that Elagolix sodium is a human GnRH receptor (GnRHR) antagonist with a Ki value of 3.7 nM[2].

Clinical Trial
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : ≥ 50 mg/mL (76.50 mM)

DMSO : 50 mg/mL (76.50 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5301 mL 7.6503 mL 15.3006 mL
5 mM 0.3060 mL 1.5301 mL 3.0601 mL
10 mM 0.1530 mL 0.7650 mL 1.5301 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (3.83 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (3.83 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (3.83 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[2]

The affinity of Elagolix sodium for hGnRH-R is determined by a competitive displacement of the radioligand GnRH from membranes prepared from HEK293 cells stably transfected with the full-length human GnRH receptor[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[2]

RBL-1 cells stably expressing the human cloned GnRH receptor are seeded into 96 well plates at a density of 15 000 cells per well in inositol-free DMEM containing 10% dialyzed FBS, 10 mM HEPES, 2 mM L-glutamine, 1 mM sodium pyruvate, 0.1 mM nonessential amino acids, and 50 μg/mL penicillin/streptomycin and are labeled for 48 h with 0.2 μCi myo-2-[3H]inositol. The cells are washed once in PBS and pretreated with assay buffer for 15 to 60 min at 37°C. The cells are then stimulated with GnRH (6 nM) in the presence or absence of Elagolix sodium and incubated for 60 min at 37°C[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

653.57

Formula

C₃₂H₂₉F₅N₃NaO₅

CAS No.

832720-36-2

SMILES

O=C([O-])CCCN[[email protected]](C1=CC=CC=C1)CN(C(N(CC2=C(C(F)(F)F)C=CC=C2F)C(C)=C3C4=CC=CC(OC)=C4F)=O)C3=O.[Na+]

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Elagolix sodium
Cat. No.:
HY-14369
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Elagolix sodium

Cat. No.: HY-14369