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Table 4: Microsomal Metabolic Stability. Metabolic stability was conducted using pooled microsomes from non-induced male rat (Sprague-Dawley) animals. The test compounds were incubated for 30 minutes at 37°C at concentrations of 1 μM. Subsequent LC/MS analysis measured disappearance of the parent molecule. The data are expressed as percent of parent remaining. Reference compounds were included for highly metabolized compounds for comparison. Metabolism rankings are based on extent of metabolism with a percent remaining breakdown as follows: 100-65= low; 65-45=moderate; <45=high. |