TABLE 1.
Inhibitors | ||||||||
---|---|---|---|---|---|---|---|---|
IC50 | ||||||||
Transporter | Substrates | Chloroquine | Hydroxychloroquine | Quinacrine | Tilorone | Pyronaridine | Cetylpyridinium | Miramistin |
µM | ||||||||
hOCT2 | [3H]Atenolol | 2.9 ± 0.02 | 5.4 ± 0.7 | 0.6 ± 0.16 | 1.11 ± 0.77 | 1.7 ± 0.5 | 22.5 ± 3.1 | 1.2 ± 0.05 |
[14C]Metformin | 15.7 ± 1.6 | 15.3 ± 5.03 | 2.08 ± 0.14 | 4.4 ± 0.34 | 5.2 ± 0.7 | 69.3 ± 18.3 | 11.5 ± 0.6 | |
[3H]MPP | 106.4 ± 19.3 | 103.7 ± 40.2 | 30.3 ± 3.9 | 60.4 ± 11.8 | 65.1 ± 17.7 | 161.8 ± 62.1 | 54.4 ± 4.8 | |
hMATE1 | [3H]Atenolol | 1.7 ± 0.19 | 2.3 ± 0.6 | 16.9 ± 6.4 | 52.9 ± 21.5 | 56.1 ± 22.1 | 20.2 ± 2.8 | 5.7 ± 0.9 |
[14C]Metformin | 2.4 ± 1.5 | 2.3 ± 0.3 | 17.13 ± 3.3 | 67.9 ± 19.4 | 84.7 ± 22.6 | 17.1 ± 6.1 | 11.98 ± 2.2 | |
[3H]MPP | 2.9 ± 1.6 | 3.6 ± 0.19 | 22.9 ± 8.2 | 84.0 ± 35 | 81.7 ± 32.3 | 19.0 ± 11.2 | 12.4 ± 2.3 | |
hMATE2K | [3H]Atenolol | 3.1 ± 2.5 | 5.5 ± 3.7 | 1.8 ± 0.8 | N/A | N/A | 23.4 ± 7.2 | 21.1 ± 6.8 |
[14C]Metformin | 11.1 ± 18.2 | 3.4 ± 4.2 | 7.3 ± 8.3 | N/A | N/A | 7.6 ± 5.4 | 29.6 ± 27.9 | |
[3H]MPP | 4.2 ± 2.4 | 6.9 ± 0.7 | 0.6 ± 0.3 | N/A | N/A | 36.3 ± 12.3 | 12.4 ± 2.8 | |
hOCT1 | [3H]Atenolol | 18.1 ± 3.7 | 39.3 ± 13.9 | 52.6 ± 7.5 | 8.4 ± 0.4 | 10.8 ± 1.6 | 7.5 ± 2.2 | 16.5 ± 4.2 |
[3H]MPP | 37.1 ± 21.4 | 46.92 ± 12.3 | 10.5 ± 1.8 | 18.3 ± 4.4 | 35.1 ± 11.2 | 30.1 ± 8.2 | 45.9 ± 4.5 |