Pioglitazone

Pioglitazone is an agonist of the peroxisome proliferator-activated receptor gamma (PPARgamma, EC50 = ~500-600 nM for both human and murine PPARgamma). It is selective for PPARgamma over PPARalpha, exhibiting low level activation of PPARalpha at 1 µM and 5.4-fold activation at a concentration of 10 µM. Pioglitazone inhibits pyruvate oxidation and glucose production in hepatocytes when used at a concentration of 10 µM. In vivo, pioglitazone (0.3-3 mg/kg per day) reduces hyperglycemia, hyperlipidemia, and hyperinsulinemia in a dose-dependent manner in male Wistar fatty rats. It reduces the number of lesions in a transgenic rat adenocarcinoma of prostate (TRAP) model. Pioglitazone (2.5 mg/kg) also decreases production of neuroinflammatory cytokines and reduces immobility in the forced swim and tail suspension tests in a mouse model of chronic mild stress, indicating antidepressant-like activity that can be reversed by the PPARgamma antagonist GW9662 (Cay-70785).Formal Name: 5-[[4-[2-(5-ethyl-2-pyridinyl)ethoxy]phenyl]methyl]-2,4-thiazolidinedione. CAS Number: 111025-46-8. Synonyms: U-72107. Molecular Formula: C19H20N2O3S. Formula Weight: 356.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 2.5 mg/ml, DMSO: 2.5 mg/ml, DMSO:PBS(pH 7.2)(1:1): 100 µg/ml. lambdamax: 267 nm. SMILES: O=C(C(S1)CC(C=C2)=CC=C2OCCC3=NC=C(CC)C=C3)[N]C1=O. InChi Code: InChI=1S/C19H19N2O3S/c1-2-13-3-6-15(20-12-13)9-10-24-16-7-4-14(5-8-16)11-17-18(22)21-19(23)25-17/h3-8,12,17H,2,9-11H2,1H3. InChi Key: XGDSMSGXFFCBJO-UHFFFAOYSA-N.