Sigma-Aldrich E17241

E17241 may be used to explore its impact on liver steatosis and adipose tissue inflammation in high-fat/high-glucose-fed mice by analyzing histological changes and gene expression profiling; to assess its cardiorenal protective effects in diabetic nephropathy and cardiomyopathy models through tissue morphology and biochemical markers.[1]

E17241 is an orally active pan-PPAR agonist (EC50 in µM = 0.29/γ, 0.88/δ(β), 3.9/α in HepG2 reporter cells) that upregulates PPAR target genes expression (ABCA1 EC50 = 626.9 nM in HepG2 reporter cells). E17241 boosts ABCA1-dependent cholesterol efflux and insulin secretion in INS-1 rat insulinoma cultures (20 nM to 10 µM) and exhibits therapeutic efficacy in diabetic mice in vivo (50 mg/kg via daily p.o.).