Table 5.
In vitro microsomal stability and cytochrome P450 (CYP) inhibition assay of compound 17a.
Microsomal stability, (%)a |
CYPs enzyme inhibition, IC50 (μM)b |
||||||||
---|---|---|---|---|---|---|---|---|---|
No | Human | Dog | Rat | Mouse | CYP3A4 | CYP1A2 | CYP2C9 | CYP2C19 | CYP2D6 |
17a | 94 | 82 | 87 | 82 | 16.2 | 10.6 | 2.9 | >20 | 8.7 |
Remaining percent of metabolism by incubation of the parent molecule (5 μM) with liver microsomes of mouse, rat, dog, and human for 60 min (duplicate).
Data were analysed by a fluorescence detection method.