Turnover rates for midazolam metabolite formation of a panel of 10 mouse CYP2C enzymes
The final concentration of midazolam in the incubations was 25 μM, and 25 pmol of enzyme was used. After a preincubation of 5 min, the reaction was started by adding a NADPH-regenerating system, and the mixture was subsequently incubated for 15 min. All values are the means of three independent experiments ± S.D.
Enzyme | v | ||
|---|---|---|---|
| 1′-OH MDZ | 4-OH MDZ | ||
| min−1 | |||
| CYP2C29 | 0.91 ± 0.04 | 0.019 ± 0.001 | |
| CYP2C37 | — | — | |
| CYP2C38 | — | — | |
| CYP2C39 | 0.10 ± 0.1 | — | |
| CYP2C44 | — | — | |
| CYP2C54 | — | — | |
| CYP2C55 | 0.016 ± 0.002 | — | |
| CYP2C65 | 0.021 ± 0.006 | 0.008 ± 0.003 | |
| CYP2C66 | — | — | |
| CYP2C70 | — | 0.28 ± 0.06 | |
—, no metabolite detected (detection limit <0.005 min−1)