Substrate specificity of OATP1B1, OATP1B3, and OATP 2B1 in transfected cells
Uptake was measured at 1 and 10 μM at 37°C for 3 min in HEK293-transfected cells and wild-type cells. The values are presented as uptake ratios (transfected/wild type). The values represent the mean of 2 to 3 replicates from a single experiment (designated with asterisks) or the mean of 2 to 3 experiments each run in duplicate or triplicate. Values in parentheses for OATP1B3 represent the uptake ratios in cells pretreated with sodium butyrate.
| Compounds | Concentration | Uptake Ratio | ||
|---|---|---|---|---|
| OATP1B1 | OATP1B3 | OATP2B1 | ||
| μM | ||||
| E-17β-G | 1 | 87 (74) | ||
| 10 | 116 (78) | |||
| ES | 1 | 6.7 | 44 | |
| 10 | 2.2 | 50 | ||
| CCK-8 | 1 | 173 (226*) | ||
| 10 | 126 (198*) | |||
| Rosuvastatin | 1 | 3.4 | 35* (16*) | 6.0 |
| 10 | 1.9 | 39* (25*) | 6.3 | |
| Midazolam | 1 | 0.92 | 1.7 (2.1*) | |
| 10 | 0.92 | 1.7 (1.9*) | ||
| Digoxin | 1 | 0.66* | 1.6 (1.8) | 1.3 |
| 10 | 0.63* | 1.9 (2.3) | 1.3 | |