Table 5.
Inhibition effects of 5j on cytochrome P450 (including CYP isozymes: CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4M).
CYP isozyme | Standard inhibitor | IC50 (μmol/L) | IC50 acceptance range (μmol/L) | Pass/No pass | Compd. | IC50 (μmol/L) |
---|---|---|---|---|---|---|
1A2 | α-Naphthoflavone | 0.290 | 0.125‒0.448 | Pass | 5j | >50.0 |
2C9 | Sulfaphenazole | 0.748 | 0.333‒0.750 | Pass | 5j | 32.9 |
2C19 | (+)-N-3-benzylnirvanol | 0.210 | 0.0928‒0.333 | Pass | 5j | >50.0 |
2D6 | Quinidine | 0.143 | 0.0928‒0.226 | Pass | 5j | >50.0 |
3A4M | Ketoconazole | 0.0410 | 0.0303‒0.0928 | Pass | 5j | >50.0 |