SR 2595 is an inverse agonist of PPARγ (IC50 = 30 nM) that represses both transactivation in a promoter:reporter assay and expression of the adipogenic marker fatty acid-binding protein 4 in differentiating murine preadipocytes. Repression of PPARγ with SR 2595 promotes osteogenesis, as measured by calcium phosphatase deposition, in cultured human mesenchymal stem cells (MSCs). SR 2595 also increases expression of bone morphogenetic proteins BMP2 and BMP6 in MSCs.
