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Table 3 Inhibitory potency of cyclosporine A, troglitazone and ketoconazole against 1 μM [ 3 H]TCA uptake into membrane vesicles (7.5 μg protein) expressing human, dog and cat BSEP/Bsep

From: The feline bile salt export pump: a structural and functional comparison with canine and human 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

  1. 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.
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BMC Veterinary Research

ISSN: 1746-6148

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