Elafibranor

Catalog No.S3720 Synonyms: GFT505

Elafibranor Chemical Structure

Molecular Weight(MW): 384.49

Elafibranor 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.

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Biological Activity

Description Elafibranor 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 ; 

PubMed: 31321239     


SIRT1-activated and autophagy-mediated effects of elafibranor on 10% HFD-sera-increased oxidative stress and apoptosis in HK-2 cells. Proteins levels in HK-2 cell lysate. ‡p<0.05 versus NC-sera group; ∗p<0.05 versus V-group; #p<0.05 versus elaf-group; †p<0.05 versus rSIRT1 group.

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

Animal Research:[2]
+ Expand
  • Animal Models: hApoE2 KI and hApoE2 KI/PPAR-α KO mice
  • Formulation: 0.1% Tween 80 and 1% carboxymethyl cellulose in 98.9% distilled water
  • 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 powder
in solvent
Synonyms GFT505

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID