A PPARα and PPARγ dual agonist
MHY908 is a dual agonist of peroxisome proliferator-activated receptor α (PPARα) and PPARγ that increases transcriptional activity of PPARα and PPARγ in a luciferase reporter assay in AC2F rat liver cells when used at a concentration of 5 µM. In vivo, MHY908 (3 mg/kg per day) reduces serum glucose, triglyceride, and insulin levels and improves hepatic steatosis by reducing hepatic triglyceride levels and lipid droplet accumulation in db/db mice and 20-month-old rats. It reduces peroxynitrite and COX-2 levels, reactive oxygen species (ROS) production, and Akt phosphorylation in isolated kidney from 20-month-old rats when administered at a dose of 3 mg/kg. MHY908 inhibits mushroom tyrosinase (IC50 = 8.19 µM). It also inhibits increases in melanin content in α-melanocyte stimulating hormone-induced B16/F10 murine melanoma cells when used at a concentration of 10 µM.
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