Kinetic parameters of MPA metabolism in HLMs, RLMs, PLMs, and recombinant CYP3A4
Km values are in micromolar, and Vm values are in picomoles per milligram per minute for liver microsomes or in minutes−1 for CYP3A4. The range of substrate concentrations was 5 to 100 μM for liver microsomes or 2 to 40 μM for CYP3A4.
Metabolite | HLMs | PLMs | RLMs | CYP3A4 | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Vm | Km | Vm/Km | Vm | Km | Vm/Km | Vm | Km | Vm/Km | Vm | Km | Vm/Km | |||||||||
| M-2 | 437 | 11.2 | 39.2 | 349 | 41.0 | 8.5 | 453 | 46.5 | 9.8 | 21.1 | 6.1 | 3.5 | ||||||||
| M-3 | 194 | 10.1 | 19.2 | 184 | 17.2 | 10.7 | 97 | 21.4 | 4.5 | 9.6 | 11.4 | 0.8 | ||||||||
| M-4 | 253 | 10.0 | 25.5 | 261 | 26.8 | 9.8 | 330 | 8.6 | 38.5 | 13.4 | 6.4 | 2.1 | ||||||||