Home Endocrinology & Hormones GNRH Receptor antagonist Elagolix Sodium

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Elagolix Sodium GNRH Receptor antagonist

Cat.No.S4896

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 GNRH Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 653.57

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (153.0 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 100 mg/mL

Ethanol : 100 mg/mL

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 653.57 Formula

C32H29F5N3O5.Na

 Storage (From the date of receipt)
CAS No. 832720-36-2 -- Storage of Stock Solutions

Synonyms NBI-56418, ABT-620 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+]

Mechanism of Action

Targets/IC50/Ki
GnRHR
(Cell-free assay)
54 pM(Kd)
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).
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).
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