Table 3.
Inhibitory potency of cyclosporine A, troglitazone and ketoconazole against 1 μM [3H]TCA uptake into membrane vesicles (7.5 μg protein) expressing human, dog and cat BSEP/Bsep
|
IC50 (μM) |
|||
|---|---|---|---|
| Human | Dog | Cat | |
| Cyclosporine A |
7.8 ± 1.2 |
3.8 ± 0.2 |
6.0 ± 0.8 |
| Troglitazone |
20.9 ± 2.9 |
23.9 ± 2.5 |
13.6 ± 4.2 |
| Ketoconazole | 20.6 ± 1.1 | 34.2 ± 2.0 | 41.8 ± 6.6 |
Inhibition curves were fitted by using GraphPad Prism 6.01 software (samples without inhibitor were set on 100%). [3H]TCA uptake in presence of ATP was corrected for uptake in presence of AMP. Measurements were performed in duplicate in four independent experiments. Statistical significance was determined by one-way ANOVA followed by the Bonferroni post-hoc test with P < 0.05 denoting a significant difference. No significant differences were found between the different species.