Home Endocrinology & Hormones GNRH Receptor antagonist Elagolix Sodium For research use only.

Elagolix Sodium

Synonyms: NBI-56418, ABT-620

Elagolix Soidum (NBI-56418, ABT-620) is a potent, selective, orally active, non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) with Kd value of 54 pM. Concentration at 10 μM shows no significant activity on ion channels, enzymes, and transporters (inhibition <50%).

Elagolix Sodium Chemical Structure

Elagolix Sodium Chemical Structure

CAS: 832720-36-2

Selleck's Elagolix Sodium has been cited by 2 publications

Purity & Quality Control

Batch: S489601 DMSO] 100 mg/mL] false] Water] 100 mg/mL] false] Ethanol] 100 mg/mL] false Purity: 99.75%
99.75

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Biological Activity

Description Elagolix Soidum (NBI-56418, ABT-620) is a potent, selective, orally active, non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) with Kd value of 54 pM. Concentration at 10 μM shows no significant activity on ion channels, enzymes, and transporters (inhibition <50%).
Targets
GnRHR [1]
(Cell-free assay)
54 pM(Kd)
In vitro
In vitro Elagolix displays high affinity in a competition binding assay for hGnRH-R (Ki = 0.90 nM) and low CYP3A4 inhibition (IC50 = 56 μM). It is a slowly disassociating antagonist exhibiting very high affinity (KD = 54 pM) and insurmountable antagonism. 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%). It does not stimulate histamine release from cultured rat peritoneal mast cells. Elagolix lacks the necessary high binding affinity to the rat GnRH receptor (Ki = 4400 nM) and it possesses high affinity at the monkey GnRH receptor (Ki = 3.3 nM)[1].
Cell Research Cell lines RBL-1 cells stably expressing the human cloned GnRH receptor
Concentrations --
Incubation Time 1 h
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℃. Cells are extracted with 10 mM formic acid at 4℃ 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.
In Vivo
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)[1].
Animal Research Animal Models Rhesus Monkey
Dosages 10 and 50 mg/kg (oral); 3 and 10 mg/kg (i.v.)
Administration p.o. or i.v.

Chemical lnformation & Solubility

Molecular Weight 653.57 Formula

C32H29F5N3O5.Na
CAS No. 832720-36-2 SDF --
Smiles CC1=C(C(=O)N(C(=O)N1CC2=C(C=CC=C2F)C(F)(F)F)CC(C3=CC=CC=C3)NCCCC(=O)[O-])C4=C(C(=CC=C4)OC)F.[Na+]
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (153.0 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 100 mg/mL

Ethanol : 100 mg/mL


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In vivo
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