Probe substrates, microsomal protein concentrations, and incubation times
| Enzyme | Probe Substrate | Microsome Concentration | Probe Substrate Concentration | Literature Km Value | Internal Standard |
|---|---|---|---|---|---|
| mg protein/ml | µM | ||||
| CYP1A2 | Phenacetin | 0.2 | 10 | 9.01, 142, 313, 544 | [2H4]Acetaminophen |
| CYP2A6 | Coumarin | 0.2 | 2.5 | 0.5 | [13C6]7-Hydroxy coumarin |
| CYP2B6 | Bupropion | 0.1 | 25 | 764, 895,1306 | [2H6]Hydroxybupropion |
| CYP2C8 | Paclitaxel | 0.2 | 10 | 4.07, 158 | Warfarin |
| CYP2C9 | Diclofenac | 0.1 | 5 | 3.49, 9.010 | [13C6]4′-Hydroxy diclofenac |
| CYP2C19 | S-Mephenytoin | 0.5 | 30 | 5112, 4213, 3114 | [2H3]4′-Hydroxy mephenytoin |
| CYP2D6 | Bufuralol | 0.2 | 5 | 1315, 4416 | [2H9]1′-Hydroxybufuralol |
| CYP2E1 | Chlorzoxazone | 0.5 | 10 | 22-4917 | [2H3]4′-Hydroxy mephenytoin |
| CYP3A4/5 | Midazolam | 0.1 | 1 | 3.3, 2.5-5.618 | [2H4]1′-Hydroxymidazolam |
| CYP3A4/5 | Testosterone | 0.2 | 30 | 50-6019, 5120 | [2H3]6β-Hydroxy testosterone |
1Tassaneeyakul et al., 1993.
2Brøsen et al., 1993.
3Venkatakrishnan et al., 1998a.
4Rodrigues et al., 1997.
5Faucette et al., 2000.
6Hesse et al., 2000.
7Li et al., 2003.
8Rahman et al., 1994.
9Cresteil et al., 1994.
10Transon et al., 1996.
11Bort et al., 1999.
12Coller et al., 1999.
13Venkatakrishnan et al., 1998b.
14Schmider et al., 1996.
15Boobis et al., 1985.
16Yamazaki et al., 1994.
17Peter et al., 1990.
18Ghosal et al., 1996.
19Draper et al., 1998.
20Kenworthy et al., 2001.