Table 1.
Summary results of Kout values of selected test compounds in Caco-2. Kout rhodamine123 was 100.0 ± 8.1 (n = 34) and 100 ± 12.1 (n = 39) for 96- and 384-well plates. Kout CMFDA was 100.0 ± 7.6 (n = 34) and 100 ± 21.7 (n = 39) for 96- and 384-well plates.
| 96 Well Plate Format | 384 Well Plate Format | Correlation 96/384 Well Plate Format | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Working Conc. | kout Rho 123 | kout CMFDA | kout Rho 123 | kout CMFDA | Ratio Kout | Transporter Interaction | ||||||||||
| pmol.min−1.mg−1 Protein | pmol.min−1.mg−1 Protein | 96/384 Wells | 96 Wells | 384 Wells | ||||||||||||
| Compounds | µM | n | mean | n | mean | n | mean | n | mean | P-gp/BCRP | MRPs | P-gp/BCRP | MRPs | P-gp/BCRP | MRPs | |
| 1 | verapamil | 50 | 34 | 33.9 ± 7.0 | 8 | 72.4 ± 6.6 | 16 | 39.3 ± 6.8 | 43 | 67.8 ± 16.5 | 0.86 | 1.07 | + | + | + | + |
| 2 | elacridar | 10 | 29 | 34.6 ± 8.9 | 8 | 71.8 ± 6.6 | 16 | 42.5 ± 9.0 | 44 | 56.4 ± 14.3 | 0.81 | 1.27 | + | + | + | + |
| 3 | MK571 | 50 | 24 | 70.9 ± 10.6 | 24 | 25.0 ± 6.6 | 16 | 59.5 ± 9.9 | 44 | 15.7 ± 5.8 | 1.19 | 1.59 | + | + | + | + |
| 4 | diazepam | 50 | 29 | 115.2 ± 18.9 | 8 | 89.2 ± 8.6 | 16 | 101.7 ± 14.6 | 44 | 95.1 ± 14.1 | 1.13 | 0.94 | − | − | − | − |
| 5 | acetanomiphen | 50 | 8 | 113.7 ± 12.6 | 8 | 90.6 ± 6.8 | 16 | 105.4 ± 8.2 | 16 | 119.1 ± 29.1 | 1.08 | 0.76 | − | − | − | − |
| 6 | amiodarone | 50 | 8 | 91.1 ± 10.2 | 8 | 83.7 ± 12.7 | 16 | 74.5 ± 12.4 | 16 | 106.5 ± 17.6 | 1.22 | 0.79 | − | − | + | − |
| 7 | cyclosporinA | 10 | 8 | 39.6 ± 9.9 | 8 | 53.1 ± 7.6 | 16 | 46.4 ± 8.1 | 16 | 42.2 ± 10.1 | 0.85 | 1.26 | + | + | + | + |
| 8 | diltiazem | 50 | 8 | 51.7 ± 5.9 | 8 | 96.4 ± 8.7 | 16 | 56.9 ± 7.1 | 16 | 87.6 ± 24.1 | 0.91 | 1.10 | + | − | + | − |
| 9 | diclofenac | 50 | 8 | 117.3 ± 15.6 | 8 | 84.1 ± 7.5 | 16 | 91.5 ± 17.4 | 16 | 118.7 ± 18.0 | 1.28 | 0.71 | − | − | − | − |
| 10 | loperamide | 50 | 8 | 42.0 ± 4.9 | 8 | 72.9 ± 4.0 | 16 | 41.6 ± 6.2 | 16 | 61.2± 16.2 | 1.01 | 1.19 | + | + | + | + |
| 11 | doxorubicin | 20 | 8 | 66.7 ± 11.0 | 8 | 66.6 ± 5.6 | 16 | 64.7 ± 6.8 | 16 | 81.3 ± 16.6 | 1.03 | 0.82 | + | + | + | − |
| 12 | phenobarbital | 50 | 8 | 107.1 ± 10.0 | 16 | 96.6 ± 11.6 | 16 | 98.5 ± 7.4 | 16 | 94.2 ± 22.4 | 1.09 | 1.03 | − | − | − | − |
| 13 | quinidine | 50 | 8 | 36.4 ± 4.2 | 8 | 77.6 ± 8.9 | 16 | 45.8 ± 6.7 | 32 | 84.7 ± 16.9 | 0.79 | 0.92 | + | +/− | + | − |
| 14 | rifampicin | 50 | 8 | 66.8 ± 4.4 | 8 | 75.5 ± 7.9 | 16 | 59.5 ± 8.0 | 16 | 76.3 ± 21.5 | 1.12 | 0.99 | + | +/− | + | +/− |
| 15 | vinblastine | 50 | 8 | 57.6 ± 3.8 | 8 | 77.6 ± 10.6 | 16 | 57.9 ± 7.6 | 32 | 81.9 ± 17.5 | 0.99 | 0.95 | + | +/− | + | − |
| 16 | tocopherol | 10 | 8 | 33.7 ± 2.7 | 8 | 88.4 ± 6.9 | 16 | 44.6 ± 6.2 | 32 | 88.8 ± 15.33 | 0.76 | 1.00 | + | − | + | − |