TABLE 1

Comparison of PF-915275 inhibition of 11bHSD1 activity in various biochemical and cell-based assays Each value represents the mean obtained from at least two independent assays. 11βHSD1-HEK293-LUC cells were incubated with PF-915275 with or without 300 nM cortisone for 6 h. Cell lysate luciferase activity was measured. Hepatocytes were pretreated with PF-915275 for 15 to 30 min before the addition of 500 nM E. Primary adipocytes were incubated with 300 nM E. Human hepatocytes were then incubated overnight, whereas monkey hepatocytes were incubated for a total of 1 h before assessing E-to-F conversion in the supernatant of treated cells.