Rosiglitazone

Rosiglitazone is an agonist of peroxisome proliferator-activated receptor gamma (PPARgamma). It activates PPARgamma1 and PPARgamma2 in reporter assays (EC50s = 30 and 100 nM, respectively). Rosiglitazone selectively activates chimeras containing the ligand-binding domains (LBDs) of PPARgamma over PPARalpha and PPARdelta in a cell-based reporter assay at 10 mM. It induces differentiation of C3H10T1/2 stem cells into adipocytes when used at a concentration of 1 µM. Rosiglitazone is also an inhibitor of long-chain acyl-CoA synthetase 4 (ACSL4, IC50 = 0.5 µM). It inhibits RSL3-induced ferroptosis in Gpx4 Cre-lox-expressing mouse embryonic fibroblasts (Pfa1) cells and Pparg knockout (KO) cells and increases survival in a Gpx4 KO mouse model of ferroptosis when used at a concentration of 0.0125 mg/ml in the drinking water. It decreases hemoglobin A1c (HbA1c) and fasting blood glucose levels in a rat model of type 2 diabetes induced by streptozotocin (STZ, Cay-13104) and a high-carbohydrate and high-fat diet when administered at a dose of 4 mg/kg. Formulations containing rosiglitazone have been used to improve glycemic control in the treatment of type 2 diabetes.Formal Name: 5-[[4-[2-(methyl-2-pyridinylamino)ethoxy]phenyl]methyl]-2,4-thiazolidinedione. CAS Number: 122320-73-4. Synonyms: BRL 49653. Molecular Formula: C18H19N3O3S. Formula Weight: 357.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMSO: 34 mg/ml, DMSO:PBS (7.2 pH) (1:3): 0.5 mg/ml, Ethanol: 1 mg/ml. lambdamax: 248, 311 nm. SMILES: O=C1NC(=O)C(S1)Cc1ccc(OCCN(C)c2ccccn2)cc1. InChi Code: InChI=1S/C18H19N3O3S/c1-21(16-4-2-3-9-19-16)10-11-24-14-7-5-13(6-8-14)12-15-17(22)20-18(23)25-15/h2-9,15H,10-12H2,1H3,(H,20,22,23). InChi Key: YASAKCUCGLMORW-UHFFFAOYSA-N.