Kinetic effects of VU0448187 heteroactivation of CYP3A4 MDZ activity
| Assay Condition | Vmax |
|---|---|
| CYP3A4 | 5.30 ± 0.26 |
| CYP3A4 + VU0448187 | 5.31 ± 0.14 |
| CYP3A4/b5 | 7.35 ± 0.43 |
| CYP3A4/b5 + VU0448187 | 10.1 ± 0.21 |
| Human liver microsomes | 1.16 ± 0.08 |
| Human liver microsomes + VU0448187 | 3.29 ± 0.16 |
Changes in Vmax for the conversion of MDZ to 1-OH-MDZ in the absence and presence of VU0448187 (10 μM) for cDNA-expressed CYP3A4 and reductase with and without cytochrome b5 and in human liver microsomes. The metabolite formation rate is expressed as picomoles per minute per picomole of P450 for the recombinant P450 or as nanomoles per minute per milligram of P450 for human liver microsomes.