Effect of substrate on OATP1B1 inhibition
Data represent individual experiments or mean ± S.D. of three experiments
| Inhibitor | IC50 | ||
|---|---|---|---|
| Pitavastatin | Estradiol-17β-glucuronide | Estrone-3-sulfate | |
| μM | |||
| Atorvastatin | 0.8 ± 0.3 | 0.6, 0.8 | 1.6, 2.4 |
| Gemfibrozil | 38 ± 2 | 11, 44 | 130, 270 |
| Glibenclamide | 2.2 ± 0.7 | 1.4, 1.4 | 21, 25 |
| Verapamil | 64 ± 15 | 32, 71 | >600, >600 |
| Simvastatin | 6 ± 3.3 | 4.4, 5.6 | 11, 14 |
| Rifampicin | 2.2 ± 1.4 | 0.3, 0.9 | 2.3, 3 |
| Ritonavir | 1 ± 0.5 | 0.7, 1 | 8.6, 5 |
| Cyclosporine A | 0.7 ± 0.2 | 0.7, 1.1 | 1.3, 1.2 |