Kinetic parameters of E217βG transport by human MRP2 and mouse Mrp2 in the presence of probenecid, sulfanitran, and sulfinpyrazone
Nonlinear regression results from the data shown in Fig. 7 are presented. Data were fitted to the Hill equation (unweighted). Modulators are used at a concentration of 500 μM.
| Control | Probenecid | Sulfanitran | Sulfinpyrazone | |
|---|---|---|---|---|
| Human MRP2 | ||||
| Vmax (pmol/mg/min) | 9683 ± 260 | 11,613 ± 137 | 7685 ± 266 | 11,294 ± 380 |
| Km (μM) | 98 ± 4 | 84 ± 2 | 24 ± 2 | 83 ± 7 |
| Hill coefficient | 1.60 ± 0.05 | 1.60 ± 0.02 | 1.19 ± 0.08 | 0.96 ± 0.03 |
| R2 | 0.9998 | 0.9999 | 0.9977 | 0.9997 |
| Mouse Mrp2 | ||||
| Vmax (pmol/mg/min) | 2621 ± 64 | 3406 ± 68 | 1971 ± 167 | N.A. |
| Km (μM) | 71 ± 3 | 48 ± 2 | 43 ± 10 | N.A. |
| Hill coefficient | 1.42 ± 0.05 | 1.11 ± 0.03 | 0.96 ± 0.1 | N.A. |
| R2 | 0.9997 | 0.9997 | 0.9953 | N.A. |
N.A., not applicable.