Table 1. Compounds that have been used for in vitro CYP450 profiling studies in micropatterned cocultures (MPCCs).
All substrates can be reconstituted in dimethyl sulfoxide (DMSO) and incubated in MPCCs at the indicated concentrations for 1 hour. The supernatants are then collected and stored at -80°C prior to LC-MS/MS analysis or luminescence analysis (for the CYP2C9-Glo and CYP3A4-Glo substrates from Promega).
| Enzyme | Concentration (μM) | Substrate | Metabolites |
|---|---|---|---|
| 1A2 | 100 | Phenacetin | Acetaminophen |
| 2A6 | 50 | Coumarin | 7-OH-coumarin |
| 2B6 | 500 | Bupropion | OH-bupropion |
| 2C8 | 30 | Paclitaxel | 6a-OH-paclitaxel |
| 2C9 | 50 | Tolbutamide | 4-OH-tolbutamide |
| 2C9 | 100 | Diclofenac | 4-OH-diclofenac |
| 2C9 | 100 | CYP2C9-Glo | Luciferin |
| 2C19 | 100 | S-mephenytoin | 4-OH-S-mephenytoin |
| 2D6 | 16 | Dextromethorphan | Dextrorphan |
| 2E1 | 300 | Chlorzoxazone | 6-OH-chlorzoxazone |
| 3A4 | 200 | Testosterone | 6b-OH-testosterone |
| 3A4 | 3 | CYP3A4-Glo (luciferin-IPA) | Luciferin |
| Phase II Metabolism | 50 | 7-OH-coumarin | 7-OH-coumarin glucuronide and 7-OH-coumarin sulfate |