Pioglitazone (hydrochloride)

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 GW 9662 (Cay-70785).Formal Name: 5-[[4-[2-(5-ethyl-2-pyridinyl)ethoxy]phenyl]methyl]-2,4-thiazolidinedione, monohydrochloride. CAS Number: 112529-15-4. Molecular Formula: C19H20N2O3S . HCl. Formula Weight: 392.9. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, DMSO:PBS (pH 7.2) (1:5): 0.15 mg/ml. lambdamax: 224, 269 nm. SMILES: CCC1=CN=C(CCOC2=CC=C(CC3SC(NC3=O)=O)C=C2)C=C1.Cl. InChi Code: InChI=1S/C19H20N2O3S.ClH/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,(H,21,22,23),1H. InChi Key: GHUUBYQTCDQWRA-UHFFFAOYSA-N.