In vitro microsomal stability and plasma protein binding of representative analogs.
Compound | Microsomal stability (%)a | Plasma protein binding rate (%) | ||
---|---|---|---|---|
Mouse | Human | Mouse | Human | |
8 | 67.7 ± 5.6 | 50.7 ± 3.2 | 84.8 ± 3.4 | 81.3 ± 2.0 |
44 | 15.7 ± 0.4 | 1.4 ± 0.1 | 94.3 ± 0.6 | 93.5 ± 0.6 |
47 | 38.6 ± 0.6 | 21.8 ± 1.4 | 89.3 ± 1.0 | 87.4 ± 2.4 |
56 | 50.6 ± 1.2 | 20.2 ± 2.3 | 96.0 ± 0.2 | 82.9 ± 0.5 |
Percentage of test compounds remaining after 30 min in mouse and human liver microsomes in the presence of NADPH (phase I stability).