Home Metabolism PPAR agonist Elafibranor For research use only.

Elafibranor

Synonyms: GFT505

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

Elafibranor Chemical Structure

CAS No. 923978-27-2

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Elafibranor Related Products

Signaling Pathway

PPAR Signaling Pathways

PPAR Signaling Pathway

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
In vitro

GFT505 is a novel PPAR modulator that shows a preferential activity on PPAR-α and concomitant activity on PPAR-δ[2].
Cell Research Cell lines hSKP-HPCs
Concentrations 30 µM
Incubation Time 24 h
Method

Cells were treated with indicated concentration of drug for 24 h.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p22phox / Nox-4 / LC3-II / Beclin-1 31321239
In Vivo
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].
Animal Research Animal Models hApoE2 KI and hApoE2 KI/PPAR-α KO mice
Dosages 30 mg/kg
Administration oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05564208 Completed
Healthy Participants
Ipsen
 October 27 2022 Phase 1
NCT05543369 Completed
Healthy Volunteers
Ipsen
 September 19 2022 Phase 1
NCT04171752 Completed
Geriatrics|Healthy
Genfit
 November 22 2019 Phase 1
NCT03883607 Terminated
Non Alcoholic Steatohepatitis
Genfit
 June 25 2019 Phase 2
NCT03844555 Completed
Renal Impairment|Renal Insufficiency|Kidney Diseases|Pharmacokinetics
Genfit
 February 28 2019 Phase 1

Chemical Information & Solubility

Molecular Weight 384.49 Formula

C22H24O4S
CAS No. 923978-27-2 SDF Download Elafibranor SDF
Smiles CC1=CC(=CC(=C1OC(C)(C)C(=O)O)C)C=CC(=O)C2=CC=C(C=C2)SC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 76 mg/mL ( (197.66 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 60 mg/mL

Water : Insoluble


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In vivo
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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.

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