LT175

LT175, a dual PPARα/γ ligand, is an orally active partial agonist against PPARγ(hPPARα:EC₅₀=0.22 μm; mPPARα:EC₅₀=0.26 μm; hPPARγ:EC₅₀=0.48 μm). LT175 interacts with PPARγ and affects the recruitment of the coregulators cyclic-AMP response element-binding protein-binding protein and nuclear corepressor 1 (NCoR1). LT175 interacts with PPARγ in a hydrophobic region called “diphenyl pocket”. LT175 has potent insulin-sensitizing effects and reduced adipogenic properties^[1]. In Vivo: LT175 (100 mg/kg/day; orally; for 3 days) induces a significant decrease in body weight (11%) and reduces fasting blood glucose, triglycerides, and free fatty acids. LT175 decreases total plasma cholesterol significantly in diet-induced Insulin-resistant mice (six-week-old C57Bl/6J male mice)^[1].