Table 4.
Conditions used for phase I/II measurements.
| Enzyme | Substrate |
C final in µM |
Measured Product | Phase II Inhibitors | Measured Wavelength |
|---|---|---|---|---|---|
| CYP 1A2 | 7-Ethoxycoumarin | 25 | 7-Hydroxycoumarin | 1.5 mM Salicylamid, 2 mM Probenecid |
355/460 nm |
| CYP 3A4 | 7-Benzyloxy-4 (trifluoromethyl) coumarin |
5 | 7-Hydroxy-4 (trifluoromethyl) coumarin |
1.5 mM Salicylamid, 2 mM Probenecid |
355/520 nm |
| CYP 2C9 | Dibenzylfluorescein | 5 | Fluorescein | 10 µM Dicumarol | 485/520 nm |
| UGT 2B7 | 4-Methylumbelliferon | 6.25 | 4-Methylumbelliferon | - | 355/460 nm |
| GST | Monochlorobimane | 50 | Monochlorobimane- glutathione conjugate | - | 355/460 nm |