Inhibitors | Substrates | ||
[3H]E2G | [3H]E1S | [3H]BSP | |
IC50 (or Km) µM | |||
E1S | 0.095 ± 0.015 | 0.271 ± 0.013b | 0.429 ± 0.175a |
611 ± 387a | |||
CsA | 0.118 ± 0.015 | 0.732 ± 0.224 | 0.694 ± 0.149 |
BSP | 0.131 ± 0.010 | 0.215 ± 0.058 | 0.327 ± 0.033b |
Ritonavir | 0.397 ± 0.023 | 46.4 ± 9.8 | 3.38 ± 0.66 |
Rifampin | 0.585 ± 0.074 | 6.96 ± 1.31 | 2.75 ± 0.62 |
Tacrolimus | 0.668 ± 0.156 | 1.78 ± 0.34 | 3.57 ± 0.43 |
Erythromycin | 4.88 ± 0.65 | 13.4 ± 4.0 | 63.3 ± 11.5 |
E2G | 7.04 ± 0.53b | 16.6 ± 2.4 | 39.3 ± 9.0 |
Ketoconazole | 9.90 ± 2.40 | 15.4 ± 3.7 | 60.9 ± 26.1 |
TCA | 19.0 ± 1.0 | 50.0 ± 4.8 | 161 ± 35 |
Verapamil | 22.3 ± 4.2 | 44.0 ± 7.3 | 84.3 ± 30.1 |
Gemfibrozil | 26.4 ± 2.1 | 381 ± 60 | 173 ± 34 |
Probenecid | 79.4 ± 5.8 | 227 ± 69 | 740 ± 181 |