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