Enzymatic constants of 8PN and IX metabolism
CYP2C8 | CYP2C19 | CYP1A2 | |
|---|---|---|---|
| 8PN-M1 | |||
| Vmax (pmol/min/pmol) | 32.7 ± 2.9a | ||
| Km (μM) | 14.8 ± 3.2 | ||
| Intrinsic clearance (μl/min/pmol) | 2.21 | ||
| 8PN-M2 | |||
| Vmax (pmol/min/pmol) | 4.64 ± 0.49a | 72.1 ± 8.4 | |
| Km (μM) | 3.72 ± 0.92 | 16.6 ± 4.6 | |
| Intrinsic clearance (μl/min/pmol) | 1.24 | 4.35 | |
| 8PN, (IX O-demethylation) | |||
| Vmax (pmol/min/pmol) | 5.47 ± 0.39a | ||
| Km (μM) | 17.77 ± 3.74 | ||
| Intrinsic clearance (μl/min/pmol) |
|
| 0.31 |
↵ a Mean ± S.D. (n = 3).