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Balaglitazone is a partial agonist of peroxisome proliferator-activated receptor (PPAR) γ [1].

PPAR plays important roles in the regulation of insulin, triglycerides and lipid metabolism. It is an attractive target for the therapy of Type II Diabetes. Balaglitazone is a partial agonist of PPARγ. The maximum inhibition of PPARγ activity by balaglitazone is 52%. Thus balaglitazone is supposed to have decreased side effects. It has showed potent effects on lowering blood glucose in various animal models [1 and 2].

In a cell-based assay using HEK293 cells transfected with fused PPARγ, treatment of balaglitazone showed sigmoid activation with an EC50 value of 1.35μM. When combined with rosiglitazone, balaglitazone at increased concentrations resulted in the reduction of rosiglitazone's activity to the level of balaglitazone alone at concentration of 100 nM [3].

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