Elafibranor

Catalog No.S3720 Synonyms: GFT505

For research use only.

Elafibranor (GFT505) is an agonist of the peroxisome proliferator-activated receptor-α(PPAR-alpha) and peroxisome proliferator-activated receptor-δ(PPAR-δ). It improves insulin sensitivity, glucose homeostasis, and lipid metabolism and reduces inflammation.

Elafibranor Chemical Structure

CAS No. 923978-27-2

Purity & Quality Control

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Biological Activity

Description Elafibranor (GFT505) is an agonist of the peroxisome proliferator-activated receptor-α(PPAR-alpha) and peroxisome proliferator-activated receptor-δ(PPAR-δ). It improves insulin sensitivity, glucose homeostasis, and lipid metabolism and reduces inflammation.
Targets
PPARα [1]
()
PPARδ [1]
()
In vitro

GFT505 is a novel PPAR modulator that shows a preferential activity on PPAR-α and concomitant activity on PPAR-δ[2].

Assay
Methods Test Index PMID
Western blot p22phox / Nox-4 / LC3-II / Beclin-1 31321239
In vivo Elafibranor (GFT505) is a dual PPARα/δ agonist that has demonstrated efficacy in disease models of nonalcoholic fatty liver disease (NAFLD)/NASH and liver fibrosis. In the rat, GFT505 concentrated in the liver with limited extrahepatic exposure and underwent extensive enterohepatic cycling. Elafibranor confers liver protection by acting on several pathways involved in NASH pathogenesis, reducing steatosis, inflammation, and fibrosis. GFT505 improved liver dysfunction markers, decreased hepatic lipid accumulation, and inhibited proinflammatory (interleukin-1 beta, tumor necrosis factor alpha, and F4/80) and profibrotic (transforming growth factor beta, tissue inhibitor of metalloproteinase 2, collagen type I, alpha 1, and collagen type I, alpha 2) gene expression[1].

Protocol (from reference)

Animal Research:[2]
  • Animal Models: hApoE2 KI and hApoE2 KI/PPAR-α KO mice
  • Dosages: 30 mg/kg
  • Administration: oral gavage
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 76 mg/mL
(197.66 mM)
Ethanol 76 mg/mL
(197.66 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 384.49
Formula

C22H24O4S

CAS No. 923978-27-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC(=CC(=C1OC(C)(C)C(=O)O)C)C=CC(=O)C2=CC=C(C=C2)SC

In vivo Formulation Calculator (Clear solution)

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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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04526665 Recruiting Drug: Elafibranor 80mg|Drug: Placebo Primary Biliary Cirrhosis Genfit September 24 2020 Phase 3
NCT04171752 Completed Drug: elafibranor Geriatrics|Healthy Genfit November 22 2019 Phase 1
NCT03883607 Terminated Drug: Elafibranor 80mg|Drug: Elafibranor 120mg Non Alcoholic Steatohepatitis Genfit June 25 2019 Phase 2
NCT03844555 Completed Drug: Elafibranor Renal Impairment|Renal Insufficiency|Kidney Diseases|Pharmacokinetics Genfit February 28 2019 Phase 1
NCT03765671 Completed Drug: Elafibranor Hepatic Impairment|Liver Disease|Pharmacokinetics Genfit|Syneos Health|University of Miami December 12 2018 Phase 1
NCT02704403 Terminated Drug: Elafibranor|Drug: Placebo Nonalcoholic Steatohepatitis (NASH) With Fibrosis Genfit March 2016 Phase 3

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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