Troglitazone

Antidiabetic thiazolidinedione. Potent and selective PPARγ ligand. Binds to the PPARγ ligand-binding domain and recruits ligand-specific transcriptional coactivators at 1µM. In skeletal muscle and adipocyte cell cultures, the EC₅₀ of troglitazone is about 10µM. Displaces [125I]SB-236636 with an IC₅₀=7.9µM. Stimulates adipogenesis and decreases osteoblastogenesis in human mesenchymal stem cells. Induces apoptosis in human vascular smooth muscle cells and inhibits the growth of a variety of human cancer cells including lung, bladder and myeloid leukemia cells. Displays an anti-invasive effect on human breast cancer cells; reduces migration, adhesion and spreading on fibronectin-coated plates. Inhibits cell growth of hematopoietic cell lines. Inhibits lamellipodia formation and actin polymerization.