Rosiglitazone

Rosiglitazone is a potent and selective PPARγ ligand. It binds to the PPARγ ligand-binding domain with a Kd of 43 nM (Lehmann et al.). It activates luciferase-based expression constructs PPARγ1 and PPARγ2 with EC₅₀ values of approximately 30 nM and 100 nM, respectively (Lehmann et al.).

MAINTENANCE AND SELF-RENEWAL

• Stimulates embryonic mouse neural stem cell proliferation and inhibits neuronal differentiation (Wada et al.).

DIFFERENTIATION

• Induces adipocyte differentiation in C3H10T1/2 stem cells (Lehmann et al.).
• Promotes endothelial differentiation, and inhibits smooth muscle differentiation, in angiogenic progenitor cells (Wang et al.).
• Stimulates adipocyte differentiation, and decreases osteogenesis, in mouse and human bone marrow-derived mesenchymal stem cells (Ali et al.; Benvenuti et al.; Lecka-Czernik et al.; Sorocéanu et al.).
• Enhances osteoclast formation in mouse bone marrow cells stimulated with RANKL and M-CSF (Wu et al.).