Compounds and concentrations tested in human hepatocytes
A range of three concentrations was selected for each compound based on literature CYP3A4 induction data for human hepatocytes. The number of concentrations was limited by hepatocyte availability. Compounds were soluble in media at the top concentrations as determined using the BD Gentest solubility scanner, which detects compound precipitates via light scatter in the relevant culture media (Coan and Shoichet, 2008).
Test Compounds | Concentrations | ||||
|---|---|---|---|---|---|
| μM | |||||
| Carbamazepine | 250 | 25 | 2.5 | ||
| CITCO | 10 | 1 | 0.1 | ||
| Clotrimazole | 3 | 0.3 | 0.03 | ||
| Dexamethasone | 250 | 25 | 2.5 | ||
| Efavirenz | 10 | 1 | 0.1 | ||
| Hyperforin | 2 | 0.2 | 0.02 | ||
| Lansoprazole | 40 | 4 | 0.4 | ||
| Mifepristone | 0.1 | 0.01 | 0.001 | ||
| Nifedipine | 50 | 5 | 0.5 | ||
| Omeprazole | 25 | 2.5 | 0.25 | ||
| Paclitaxel | 50 | 5 | 0.5 | ||
| Phenobarbital | 2000 | 200 | 20 | ||
| Phenytoin | 250 | 25 | 2.5 | ||
| Pioglitazone | 50 | 5 | 0.5 | ||
| Quinidine | 250 | 25 | 2.5 | ||
| Reserpine | 10 | 1 | 0.1 | ||
| Rifabutin | 10 | 1 | 0.1 | ||
| Rifampicin | 10 | 1 | 0.1 | ||
| Rifapentine | 10 | 1 | 0.1 | ||
| Ritonavir | 1 | 0.1 | 0.01 | ||
| β-Naphthoflavone | 25 | 2.5 | 0.25 | ||
| Sulfinpyrazone | 150 | 15 | 1.5 | ||
| Troglitazone | 5 | 0.5 | 0.05 | ||
| Troleandomycin | 20 | 2.0 | 0.2 | ||
| Verapamil | 40 | 4 | 0.4 | ||