Elafibranor
PPARα/δ agonist / Elafibranor is a dual PPARalpha/delta agonist (EC50 PPARalpha = 10-20 nM; PPARdelta = 100-150 nM).1 It was able to decrease plasma triglycerides levels1, increase HDL cholesterol levels in human studies1, and improve hepatic and peripheral insulin sensitivity2. Elafibranor’s antidiabetic effects in db/db were without the adverse cardiac effects seen in PPARgamma agonism.3 Elafibranor has also been shown to have therapeutic promise in the treatment of nonalcoholic steatohepatitis (NASH).4-6
Biochemicals & reagents
923978-27-2
GFT505
1) Cariou et al. (2011) Effects of the New Dual PPAR?/? Agonist GFT505 on Lipid and Glucose Homeostasis in Abdominally Obese Patients With Combined Dyslipidemia or Impaired Glucose Metabolism; Diabetes Care 34 2008 2) Cariou et al. (2013) Dual peroxisome proliferator receptor ?/? agonist GFT505 improves hepatic and peripheral insulin sensitivity in abdominally obese subjects; Diabetes Care 36 2923 3) Hanf et al. (2014) The dual peroxisome proliferator-activated alpha/delta agonist GFT505 exerts anti-diabetic effects in db/db mice without peroxisome proliferator-activated receptor gamma-associated adverse cardiac effects.; Diab. Vasc. Dis. Res. 11 440 4) Staels et al. (2013) Hepatoprotective effects of the dual peroxisome proliferator-activated receptor alpha-delta agonist, GFT505, in rodent models of nonalcoholic fatty liver disease/nonalcoholic steatohepatitis; Hepatology 58 1941 5) Ratziu et al. (2016) Elafibranor, an Agonist of the Peroxisome Proliferator-Activated Receptor-? and -?, Induces Resolution of Nonalcoholic Steatohepatitis Without Fibrosis Worsening.; Gastroenterology. 39 2951 6) Boeckmans et al. (2019) Elafibranor restricts lipogenic and inflammatory responses in a human skin stem cell-derived model of NASH.; Pharmacol. Res. 114 377
-20°C
TARGET: Transcription factor -- PATHWAY: Fatty acid metabolism; Cholesterol metabolism; PPAR; Transcription -- DISEASE AREA: Diabetes; InflammationLiver disease; Kidney disease