Table 2.
Inhibition of OATP1B1- and OATP1B3-Mediated Fluorescein-Methotrexate (FMTX) Uptake by Prestwick Library Compounds
| Compound | IC50 on OATP1B1 (µM) | IC50 on OATP1B3 (µM) |
|---|---|---|
| 2-aminobenzenesulfonamide | > 100 | > 100 |
| Aconitine | > 100 | No inhibition |
| Beclomethasone | 6.7 ± 1.2 | 1.4 ± 0.4 |
| Bromocryptine | 0.7 ± 0.08 | 1.8 ± 0.3 |
| Captopril | No inhibition | No inhibition |
| Ergocryptine | 0.8 ± 0.2 | 2.2 ± 1.2 |
| Estropipate | 0.06 ± 0.01 | 19.3 ± 6.3 |
| Etomidate | > 100 | > 100 |
| Fipexide | 34.5 ± 6.8 | > 100 |
| Metronidazole | > 100 | > 100 |
| Moricizine | 8.1 ± 1.9 | 2.7 ± 0.4 |
| Niflumic acid | 3.7 ± 1.4 | 22.0 ± 6.8 |
| Ramipril | 4.0 ± 0.5 | 3.3 ± 0.3 |
| Repaglinide | 1.1 ± 0.2 | 4.8 ± 0.7 |
| Resveratrol | 11.2 ± 2.0 | 23.7 ± 2.5 |
| Rifampicin | 1.3 ± 0.2 | 1.5 ± 0.5 |
| Trifluridine | No inhibition | No inhibition |
| Ursolic acid | 12.5 ± 1.9 | 2.3 ± 0.03 |
Results are means ± SE of at least three independent experiments.