Cytochrome P450 Inhibition
Currently under Redevelopment
Because of the important role of Cytochrome p450 enzymes in drug metabolism, it is important to assess the ability of lead compounds to inhibit specific cytochrome p450 enzymes to avoid potential drug-drug interactions where one drug may affect the metabolism of another. This assay is only recommended for advanced leads.
Typical Assay Conditions
| Isoform | Source | Substrate | Positive Inhibitor |
|---|---|---|---|
| 1A2 | BD Bioscience Supersome | phenacetin | furfylline |
| 2C9 | BD Bioscience Supersome | diclofenac | sulfaphazole |
| 2C19 | BD Bioscience Supersome | mephenytoin | ticlopidine |
| 2D6 | BD Bioscience Supersome | bufuralol | quinidine |
| 3A4 | BD Bioscience Supersome | Under-redevelopment | ketaconazole |
Assay Format: 9 point curve for IC50 determination
Analysis: LC-MS/MS of specific drug probe metabolite
Requirements: 150 microliters of 10 mM drug stock
