Pioglitazone

Pioglitazone selectively activates PPARγ-1. It is about one tenth as potent as rosiglitazone (EC₅₀~500nM for human and mouse PPARγ). 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 1µM and 5.4- and 4.2-fold activation, respectively, at a concentration of 10µM.

Thiazolidinediones (TZDs) are a group of structurally related PPARγ agonists with anti-diabetic actions in vivo. Rosiglitazone (Prod. No. ALX-350-125) is a prototypical TZD and has served as a reference compound for this class of PPARγ ligands.