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Elagolix sodium

Cat. No. M9196

All AbMole products are for research use only, cannot be used for human consumption.

Elagolix sodium Structure
Synonym:

NBI56418; ABT-620

Size Price Availability Quantity
5mg USD 55  USD55 In stock
10mg USD 80  USD80 In stock
25mg USD 150  USD150 In stock
50mg USD 260  USD260 In stock
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Quality Control & Documentation
Biological Activity

Elagolix displays high affinity in a competition binding assay for hGnRH-R (Ki = 0.90 nM) and low CYP3A4 inhibition (IC50 = 56 μM). Elagolix is highly selective at hGnRH-R, its wider receptor selectivity is tested at a concentration of 10 μM in a panel of radioligand binding assays for 100 off-target receptors, ion channels, enzymes, and transporters, and significant activity is not observed (inhibition <50%).

In vivo, oral administration of Elagolix suppresses luteinizing hormone in castrated macaques. Elagolix shows good efficacy in suppressing luteinizing hormone in monkeys and exhibits high oral bioavailability in dogs (~100% when dosed via oral gavage at 50 mg/kg).

Protocol (for reference only)
Cell Experiment
Cell lines RBL-1 cells stably expressing the human cloned GnRH receptor
Preparation method 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 (140 mM NaCl, 4 mM KCl, 20 mM HEPES, 8.3 mM glucose, 1 mM MgCl2, 1 mM CaCl2, 10 mM LiCl, and 0.1% BSA) for 15-60 min at 37 °C. The cells are then stimulated with GnRH (6 nM) in the presence or absence of antagonist and incubated for 60 min at 37°C. Cells are extracted with 10 mM formic acid at 4°C for 30 min, and the lysate is loaded onto Millipore plates containing 20 μg of Dowex AG1-X8 resin. The plate is washed once in H2O and once in 60 mM ammonium formate/5 mM sodium tetraborate, and inositol phosphates are eluted with 1 M ammonium formate/0.1 M formic acid. The eluate is transferred to a Lumaplate and counted in a TopCount NXT.
Concentrations -
Incubation time 1 h
Animal Experiment
Animal models Rhesus Monkey
Formulation water or 5% cromophore (For i.v. formulation); a sterile water solution (For oral formulation)
Dosages 10 and 50 mg/kg (oral); 3 and 10 mg/kg (i.v.)
Administration p.o. or i.v.
Chemical Information
Molecular Weight 653.57
Formula C32H29F5N3O5.Na
CAS Number 832720-36-2
Solubility (25°C) DMSO: ≥ 85 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Chen C, et al. J Med Chem. 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.

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Keywords: Elagolix sodium, NBI56418; ABT-620 supplier, Estrogen Receptor, inhibitors, activators

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