Thiazolidinediones (TZDs) are a group of structurally related peroxisome proliferator-activated receptor γ (PPARγ) agonists with antidiabetic actions in vivo.{7575,8930} Rosiglitazone is a prototypical TZD that has served as a reference compound for this class.{8461} It is a potent and selective PPARγ ligand that binds to the PPARγ ligand-binding domain with a Kd value of 43 nM.{8461} It activates luciferase-based expression constructs PPARγ1 and PPARγ2 with EC50 values of approximately 30 nM and 100 nM, respectively.{8461} Rosiglitazone is active in vivo as an antidiabetic agent in the ob/ob mouse model, and has been used as an oral hypoglycemic agent in the treatment of type 2 diabetes in humans for many years.
产品描述
A potent and selective PPARγ ligand, binding to the PPARγ ligand-binding domain with a Kd value of 43 nM