Table 3.
In vitro microsomal stabilities of compounds 7a, 7k, 12a, 12b, 19a, and 19b in liver microsomes from mice, rats, or humans
Compounds | Metabolic stability in mouse | Metabolic stability in rat | Metabolic stability in human | |||
---|---|---|---|---|---|---|
t1/2 (h) | Clint (μL/min/mg) | t1/2 (h) | Clint (μL/min/mg) | t1/2 (h) | Clint (μL/min/mg) | |
7a | 0.8 | 27.8 | 1.0 | 22.6 | 1.9 | 12.0 |
7k | 1.0 | 24.3 | 0.9 | 24.8 | 2.3 | 10.0 |
12a | 0.7 | 35 | 1.3 | 18.0 | 1.3 | 17.5 |
12b | 1.1 | 21.6 | 1.6 | 14.2 | 1.5 | 15.7 |
19a | >4 | 5.5 | 2.5 | 9.2 | >4 | 3.2 |
19b | 1.2 | 19.9 | 0.6 | 36.7 | 1.4 | 16.3 |
Verapamil | 0.1 | 192.5 | 0.2 | 100.4 | 0.3 | 85.6 |