Elafibranor

Catalog No.S3720 Batch:S372004

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Technical Data

Formula

C22H24O4S
Molecular Weight 384.49 CAS No. 923978-27-2
Solubility (25°C)* In vitro DMSO 77 mg/mL (200.26 mM)
Ethanol 13 mg/mL (33.81 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.48mg/ml Taking the 1 mL working solution as an example, add 50 μL of 9.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
3.85mg/ml Taking the 1 mL working solution as an example, add 50 μL of 77 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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].
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)

Cell Assay:

[3]
  • Cell lines

    hSKP-HPCs

  • Concentrations

    30 µM

  • Incubation Time

    24 h

  • Method

    Cells were treated with indicated concentration of drug for 24 h.
Animal Study:

[2]
  • Animal Models

    hApoE2 KI and hApoE2 KI/PPAR-α KO mice

  • Dosages

    30 mg/kg

  • Administration

    oral gavage

Selleck's Elafibranor has been cited by 2 publications

A new NRF2 activator for the treatment of human metabolic dysfunction-associated fatty liver disease [ JHEP Rep, 2023, 5(10):100845] PubMed: 37663119
A new NRF2 activator for the treatment of human metabolic dysfunction-associated fatty liver disease [ JHEP Rep, 2023, 5(10):100845] PubMed: 37663119

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.