Table 2. Kinetic parameters for the uptake of HMME isomers into hepatocytes and hOATP-expressing HEK293 cells. Data are shown as the mean±SD. n=3.
| Compound | Transporter/hepatocytes | Kinetic model | Km (μmol/L) | Vmax (pmol·min−1·mg−1) | Vmax/Km ratio (μL·min−1·mg−1) | h |
|---|---|---|---|---|---|---|
| HMME-1 | Rat hepatocytes | Allosteric sigmoidal | 0.63±0.04 | 64.8±2.2 | 103±6 | 2.74±0.49 |
| Human hepatocytes | Michaelis-Menten | 4.45±1.05 | 50.3±4.6 | 11.3±1.8 | – | |
| OATP1B1 | Allosteric sigmoidal | 5.61±0.59 | 160±9.5 | 28.6±1.6 | 1.73±0.16 | |
| OATP1B3 | Michaelis-Menten | 1.51±0.31 | 37.0±3.5 | 24.5±2.9 | – | |
| OATP2B1 | Allosteric sigmoidal | 1.48±0.12 | 61.4±2.2 | 41.4±2.6 | 1.48±0.22 | |
| HMME-2 | Rat hepatocytes | Michaelis-Menten | 3.77±0.85 | 269±33 | 71.4±7.4 | – |
| Human hepatocytes | Michaelis-Menten | 0.98±0.08 | 62.8±1.6 | 63.8±4.3 | – | |
| OATP1B1 | Michaelis-Menten | 0.63±0.11 | 72.6±4.5 | 115±14.1 | – | |
| OATP1B3 | Michaelis-Menten | 0.58±0.09 | 23.4±1.0 | 40.1±5.1 | – | |
| OATP2B1 | Michaelis-Menten | 1.92±0.23 | 178±6.0 | 92.3±8.9 | – |