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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO ≥ 20 mg/mL|
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.
|Related PPAR Products|
Seladelpar (MBX-8025; RWJ-800025) is a selective peroxisome proliferator-activated receptor (SPPAR) -δ receptor agonist.
EHP-101 (VCE-004.8) is an orally active, specific PPARγ and CB2 receptor dual agonist.
Lanifibranor (IVA-337) is a peroxisome proliferator-activated receptors (PPAR) agonist, with EC50s of 1.5, 0.87 and 0.21 μM for human PPARα, PPARσ and PPARγ, respectively.
Balaglitazone is an agonist of peroxisome proliferator-activated receptor (PPAR) γ, with an EC50 of 1.351 μM for human PPARγ.
SR-18292 is a PPAR gamma coactivator-1α (PGC-1α) inhibitor, which increases PGC-1α acetylation, suppresses gluconeogenic gene expression.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.