Formulation: A crystalline solid
Formal Name: 5-[[4-[2-(methyl-2-pyridinylamino)ethoxy]phenyl]methyl]-2,4-thiazolidinedione, monopotassium salt
Purity: ≥98%
Formula Markup: C18H18N3O3S • K
Formula Weight: 395,5
Shelf life (days): 730
CAS Number: 316371-84-3
Notes: Rosiglitazone is an agonist of peroxisome proliferator-activated receptor γ (PPARγ).{8461} It activates PPARγ1 and PPARγ2 in reporter assays (EC50s = 30 and 100 nM, respectively). Rosiglitazone selectively activates chimeras containing the ligand-binding domains (LBDs) of PPARγ over PPARα and PPARδ 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), inhibits RSL3-induced ferroptosis in 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.{60818,43378} It decreases hemoglobin A1c (HbA1c) and fasting blood glucose levels in a rat model of type 2 diabetes induced by streptozotocin (STZ; Item No. 13104) and a high-carbohydrate and high-fat diet when administered at a dose of 4 mg/kg.{16286} Formulations containing rosiglitazone have been used to improve glycemic control in the treatment of type 2 diabetes.
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