Fig. 8.
Assessment of metabolic stability of 4a in human liver microsomes. (A) 4a (10 μM) was incubated in the presence of human liver microsomes (1.0 mg/mL; HLMs;-△-), HLMs plus NADPH (1 mM; -●-), or buffer only (0.1 M KH2PO4, pH 7.4; –□–), for 0, 15, 30 or 60 min at 37 °C. The data are expressed as percent of parent compound (4a) remaining at each time compared with time 0 min, and represent the mean ± SD of n = 3 or 4 independent determinations. (B) Representative stacked HPLC-fluorescence traces of supernatants from mixtures containing 4a (10 μM) and HLMs (1.0 mg/mL), incubated for 0, 15, 30 or 60 min at 37 °C. M, 4a metabolite.