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Elafibranor

Cat. No. M9476
Elafibranor Structure
Synonym:

GFT505

Size Price Availability Quantity
5mg USD 60 In stock
10mg USD 90 In stock
50mg USD 360 In stock
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Quality Control
Biological Activity

Elafibranor (also known as GFT-505) is a dual PPARα/δ agonist with EC50s of 45 and 175 nM, respectively. Elafibranor (GFT505) treatment improves glucose control and plasma lipids in diabetic db/db mice. A significant dose-dependent reduction of hepatic expression of the key gluconeogenic enzymes glucose 6-phosphatase (G6Pase), PEPCK, and fructose 1,6-bisphosphatase 1 (FBP1) is observed with Elafibranor.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 384.49
Formula C22H24O4S
CAS Number 923978-27-2
Purity 98.43%
Solubility DMSO ≥ 20 mg/mL
Storage at -20°C
References

Elafibranor, an Agonist of the Peroxisome Proliferator-Activated Receptor-α and -δ, Induces Resolution of Nonalcoholic Steatohepatitis Without Fibrosis Worsening.
Ratziu V, et al. Gastroenterology. 2016 May;150(5):1147-1159.e5. PMID: 26874076.

The dual peroxisome proliferator-activated receptor alpha/delta agonist GFT505 exerts anti-diabetic effects in db/db mice without peroxisome proliferator-activated receptor gamma-associated adverse cardiac effects.
Hanf R, et al. Diab Vasc Dis Res. 2014 Nov;11(6):440-7. PMID: 25212694.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Elafibranor, GFT505 supplier, PPAR, inhibitors

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