Kinetic parameters for the formation of the metabolites of tazofelone in human liver microsomes
| Metabolite | Km (μM) | Vmax (nmol/min/mg protein) | CLint(site 1) (ml/min/mg protein) | CLint(site 2) (ml/min/mg protein) |
|---|---|---|---|---|
| Sulfoxide | 12.4 ± 1.4 | 0.27 ± 0.12 | 0.022 | — |
| Quinol | 7.5 ± 1.6 | 0.17 ± 0.02 | 0.023 | 0.002 |
Formation rates of metabolites were measured as described inMaterial and Methods. Km andVmax values were determined by nonlinear regression as described in Material and Methods. Incubations were performed in duplicate using tazofelone concentrations ranging from 3.9 μM to 1500 μM.