Comparison of the apparent inhibition constants (Ki app) and the kinetic parameters (KM) of various organic compounds
| Compound | Ki app | KM3-a | ||
|---|---|---|---|---|
| Hepatocytes | Oatp 1 | Oatp 1 | Oatp 2 | |
| μM | μM | μM | μM | |
| Cholyltaurine | 15 ± 7 | 9.5 ± 1.5 | 19–503-a | 353-a |
| BSP | 0.26 ± 0.05 | 0.8 ± 0.2 | 1.5–3.33-a | N.T. |
| SLCT | 0.31 ± 0.05 | 0.5 ± 0.2 | 63-a | N.T. |
| Estron-3-sulfate | 4.2 ± 1.5 | 5.6 ± 2.8 | 4.5–123-a | 11 |
| Bumetanide | 21.8 ± 4.4 | 34 ± 20 | ||
| Probenecide | 54 ± 20 | 42 ± 2 | ||
| Phenolred | 122 ± 83 | 38 ± 10 | ||
| Ouabain | 1400 ± 170 | 1230 ± 245 | 1700–30003-a | 4703-a |
| Verapamil | 21.3 ± 6.7 | 40.5 ± 12.3 | ||
| Digoxin | 93 ± 32 | 103 ± 28 | N.T. | 0.243-a |
| NMN | N.S. at 100 | N.D. | ||
| α-Ketoglutarate | N.S. at 5000 | N.D. | N.T. | N.T. |
| p-Aminohippurate | N.S. at 100 | N.D. | N.T. | N.T. |
| Geneticin sulfate | N.S. at 577 | N.D. | ||
| 5-Sulfosalicylate | N.S. at 100 | N.D. | ||
Apparent inhibition constants (Ki app) were determined as described in Table 2.
N.S., no significant inhibition at the indicated concentration; N.T., not transported; N.D., not determined in this study.
↵3-a KM values are from Reichel et al. (1999).