Peroxisome proliferator-activated receptors (PPARs) are activated by fatty acids and eicosanoids as well as antidyslipidemic agents. Among the receptor isotypes, PPARα demonstrates a particular role in fatty acid oxidation, whereas PPARγ is known to be involved in adipocyte differentiation and lipid storage. MHY908 is a dual agonist of PPARα and PPARγ. MHY908 has been shown to enhance the binding and transcriptional activity of PPARα and PPARγ in AC2F cells (5 μM) more potently than fenofibrate or rosiglitazone and to reduce serum glucose, triglyceride, and insulin levels in db/db mice (3 mg/kg). It is also reported to improve hepatic steatosis by enhancing CPT-1 levels and to reduce endoplasmic reticulum stress and JNK activation in the livers of db/db mice, leading to reduced insulin resistance.
