In vitro activity: Compounds (including CAY10602/compound 1) with SIRT1-activating properties have a significant effect on fat mobilization in differentiated adipocytes, and these compounds (including CAY10602) have antiobesity and/or antidiabetic properties. Compounds (including CAY10602) with SIRT1 activating potential exert strong suppression of TNF-α release at concentrations between 20 and 60 μM.
Cell Assay: 3T3L1 mouse fibroblasts and THP-1 leukemia cells are used and cultured following the supplier’s recommendations.THP-1 cells are treated first with representative compounds (including CAY10602/compound 1) followed by addition of lipopolysaccharide(LPS). THP-1 cells are plated at a density of 1.2×106 cells/mL in 0.4 mL (0.5×106 cells/treatment) in 24-well culture plates. The cells are preincubated with representative test compounds (including CAY10602) at 2 concentrations (20 or 60 μM) for 1 h under general tissue culture conditions. |