Pioglitazone hydrochloride (AD 4833) is the hydrochloride salt of an orally-active thiazolidinedione with antidiabetic properties and potential antineoplastic activity.

PPARγ (human):0.93 μM (EC50), PPARγ (mouse):0.99 μM (EC50), PPARδ:0.01 μM (EC50, human)

In male obese rats, oral administration of Pioglitazone (0.3-3 mg/kg) over a period of 7 days resulted in a dose-dependent reduction of hyperglycemia, hyperlipidemia, and hyperinsulinemia.

Pioglitazone protects dopaminergic neurons from LPS-induced damage by inhibiting the expression of iNOS and the production of NO. It also suppresses the phosphorylation of p38 protein induced by lipopolysaccharides.

In order to evaluate cell proliferation, HIT-T15 cells are seeded on 96-well plates (3×104 cells/well) and cultured for 5 days as described. Viable cells are determined using the Cell Titer 96 Aqueous One Solution Cell Proliferation Assay. To evaluate cell apoptosis and cell necrosis, HIT-T15 cells are plated on 6-well dishes (7×105 cells/well) for 5 days in standard conditions (CTR) or in the presence of AGEs (AGEs) with or without Pioglitazone (0.5 or 1 μM) or AG (1 mM). They are then processed to measure both the activity of caspase-3 and the activity of lactate dehydrogenase (LDH) (a stable cytosolic enzyme that is a marker of cell membrane damage and cell death due to necrosis) using Cytotox 96 Non Radioactive Cytotoxicity Assay[2].