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

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability

Quality Control

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

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+]

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

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
GnRHR [1]
(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)[1].
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].
References

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