Rosiglitazone

Rosiglitazone, also known as BRL 49653, is a potent and selective agonist for PPARγ (Peroxisome proliferator-activated receptor) with an EC50 of 43 nM. PPARγ plays a functional role in adipogenesis, it belongs to a group of nuclear receptor proteins that are essential to the regulation of cellular differentiation, development and metabolism. Rosiglitazone binds to the PPAR receptors in fat cells and making the cells more responsive to insulin. It activates luciferase-based expression constructs PPARγ1 and PPARγ2 with EC50 values of approximately 30 nM and 100 nM, respectively. Rosiglitazone induced adipocyte differentiation in pluripotent C3H10T1/2 stem cells. Rosiglitazone suppressed the activity of complex I of the MRC in ob/ob mice, but did not affect beta-oxidation.