Thiazolidinediones (TZDs) are a group of structurally related PPARγ agonists with anti-diabetic actions in vivo.{7575,8930} Rosiglitazone (BRL49653) is a prototypical TZD and has served as a reference compound for this class of PPARγ ligands.{8461} Pioglitazone is a closely related TZD which also selectively activates PPARγ-1. Pioglitazone is about one tenth as potent as rosiglitazone, with an EC50 of about 500-600 nM for both human and mouse PPARγ.{10857,10670} In a transactivation assay using COS-1 cells transfected with full length human PPARα and RXRα, pioglitazone and rosiglitazone exhibit low level activation of PPARα at 1 µM and 5.4- and 4.2-fold activation, respectively, at a concentration of 10 µM.{10857}
产品描述
A thiazolidinedione that selectively activates PPARγ-1 with an EC50 of 500-600 nM for both human and mouse PPARγ; exhibits low level activation of PPARα in a transactivation assay using COS-1 cells transfected with full length human PPARα and RXRα
