Table 11. . In vitro microsomal stability assay of compound 6f.
Compound | C (μM) | Test species | NADPH-dependent CLint† (μl/min/mg) | NADPH-dependent T1/2‡ (min) | NADPH-free CLint† (μl/min/mg) | NADPH-free T1/2‡ (min) |
---|---|---|---|---|---|---|
6f | 1 | Human | 21.7 | 106 | <12.8 | >180 |
Verapamil | 1 | Human | 123 | 18.7 | <12.8 | >180 |
Dextromethorphan | 1 | Human | 24.3 | 94.9 | <12.8 | >180 |
Microsomal intrinsic clearance = ln(2)/(T1/2[microsomal protein]).
Half-life = 0.693/-k, where k is the rate constant.