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Elagolix Sodium

Name: Elagolix Sodium
Brand: Selleck Chemicals
SKU: S4896
Rating: 5 (2 reviews)

Synonyms: NBI-56418, ABT-620

Catalog No.S4896 Purity: 99.75%

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

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

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.

References

[1] Chen C, et al. J Med Chem. 2008, 51(23):7478-85.

Chemical Information & 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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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% DMSO + % + % Tween 80 + % ddH₂O

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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