Rosiglitazone-d3 is intended for use as an internal standard for the quantification of rosiglitazone by GC- or LC-MS. Rosiglitazone is a thiazolidinedione agonist of peroxisome proliferator-activated receptor γ (PPARγ) that binds to the ligand binding domain (LBD) of PPARγ with a Kd value of 43 nM.1 It selectively activates chimeras containing the LBDs of PPARγ over PPARα and PPARδ in a cell-based reporter assay when used at a concentration of 10 mM. Rosiglitazone also activates full-length PPARγ1 and PPARγ2 in a reporter assay (EC50s = 30 and 100 nM, respectively). It induces differentiation of C3H10T1/2 stem cells to adipocytes when used at a concentration of 1 μM. Rosiglitazone (4 mg/kg) decreases hemoglobin A1c (HbA1c) and fasting blood glucose levels in a rat model of type 2 diabetes induced by streptozotocin and a high-carbohydrate/high-fat diet.2 It also inhibits increases in contusion volume, macrophage infiltration and activation of microglia, and expression of IL-6, MCP1, ICAM1, caspase-3, and Bax in mouse cerebral cortex in a model of traumatic brain injury induced by controlled cortical impact when administered at a dose of 6 mg/kg.3 Formulations containing rosiglitazone have been used to improve glycemic control in the treatment of type 2 diabetes.
1.Lehmann, J.M., Moore, L.B., Smith-Oliver, T.A., et al.An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor γ (PPARγ)J. Biol. Chem.270(22)12953-12956(1995) 2.Zhou, J.Y., Zhou, S.W., Zhang, K.B., et al.Chronic effects of berberine on blood, liver glucolipid metabolism and liver PPARs expression in diabetic hyperlipidemic ratsBiological and Pharmaceutical Bullentin31(6)1169-1176(2008) 3.Yi, J.-H., Park, S.-W., Brooks, N., et al.PPARγ agonist rosiglitazone is neuroprotective after traumatic brain injury via anti-inflammatory and anti-oxidative mechanismsBrain Res.1244164-172(2008)