Assessment of EE2-Sul as an OCT2, OAT1, and MATE1 substrate
The details of measurement are described under Materials and Methods.
| Transporter | Compound | Uptake by Cells (pmol/mg/3 min) | |
|---|---|---|---|
| OCT2 | Mock/HEK-293 cells | OCT2/HEK-293 cells | |
| 1 μM [3H]MPP | 4.5 ± 0.4 | 362.6 ± 37.0a | |
| 1 μM [3H]MPP + 200 μM imipramine | 3.3 ± 0.4 | 17.2 ± 0.9b | |
| 1 μM [3H]EE2-Sul | 3.6 ± 0.5 | 3.7 ± 0.5 | |
| 1 μM [3H]EE2-Sul + 200 μM imipramine | 3.8 ± 0.4 | 4.6 ± 0.5 | |
| OAT1 | Mock/MDCK cells | OAT1/MDCK cells | |
| 1 μM [3H]PAH | 0.77 ± 0.14 | 15.9 ± 2.2c | |
| 1 μM [3H]PAH + 50 μM BSP | 0.91 ± 0.15 | 1.70 ± 0.12d | |
| 1 μM [3H]EE2-Sul | 3.8 ± 0.4 | 3.5 ± 0.3 | |
| 1 μM [3H]EE2-Sul + 50 μM BSP | 3.1 ± 0.2 | 3.1 ± 0.1 | |
| MATE1 | Mock/HEK-293 cells | MATE1/HEK-293 cells | |
| 1 μM [3H]MPP | 8.55 ± 0.92 | 58.6 ± 2.7e | |
| 1 μM [3H]MPP + 1 μM pyrimethamine | 8.48 ± 2.62 | 8.14 ± 0.98f | |
| 1 μM [3H]EE2-Sul | 3.7 ± 0.2 | 3.8 ± 0.2 | |
| 1 μM [3H]EE2-Sul + 1 μM pyrimethamine | 3.4 ± 0.7 | 3.9 ± 0.4 | |
↵a p < 0.01 vs. 1 μM [3H]MPP uptake by mock/HEK-293 cells.
↵b p < 0.01 vs. 1 μM [3H]MPP uptake by OCT2/HEK-293 cells.
↵c p < 0.01 vs. 1 μM [3H]PAH uptake by mock/MDCK cells.
↵d p < 0.01 vs. 1 μM [3H]PAH uptake by OAT1/MDCK cells.
↵e p < 0.01 vs. 1 μM [3H]MPP uptake by mock/HEK-293 cells.
↵f p < 0.01 vs. 1 μM [3H]MPP uptake by MATE1/HEK-293 cells.