LT175, a dual PPARα/γ ligand, demonstrates potent insulin-sensitizing effects while exhibiting reduced adipogenic properties. This compound is an orally active partial agonist targeting PPARγ, with EC50 values of 0.22 μm for hPPARα, 0.26 μm for mPPARα, and 0.48 μm for hPPARγ. LT175 specifically interacts with PPARγ, influencing the recruitment of coregulators such as the cyclic-AMP response element-binding protein-binding protein and nuclear corepressor 1 (NCoR1). Additionally, LT175's interaction with PPARγ occurs within a hydrophobic region known as the "diphenyl pocket" [1].

PPARα (mouse):0.26 μM (EC50), PPARγ (human):0.48 μM (EC50), PPARα (human):0.22 μM (EC50)

LT175 (100 mg/kg/day; orally; for 3 days) significantly reduce the 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].