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