Thiazolidinediones are a group of structurally related peroxisome proliferator-activated receptor γ (PPARγ) agonists with antidiabetic actions in vivo. Rosiglitazone is a prototypical thiazolidinedione and has served as a reference compound for this class. Rosiglitazone is a potent and selective PPARγ ligand. It binds to the PPARγ ligand-binding domain with a Kd of 43 nM. It activates a luciferase-based PPARγ expression construct with an EC50 of about 1.0 μM. Rosiglitazone is active in vivo as a antidiabetic agent in the ob/ob mouse model, and has been used as an oral hypoglycemic agent in the treatment of Type II diabetes in humans for many years. The potassium salt of rosiglitazone is a formulation designed to provide better aqueous solubility than the parent compound.
