Fig. 5 Concentration-dependent inhibition of OATP1B1, OATP1B3, and OATP2B1-mediated transport by PRA determined in a cell-based functional assay using radiolabeled [3H]BSP and stably transfected HEK-OATP1B1 (IC50: 3.25 µM ± 0.09 µM; A), HEK-OATP1B3 (IC50: 2.55 µM ± 0.21 µM; B), and HEK-OATP2B1 (IC50: 1.31 µM ± 0.06 µM; C) as well as respective HEK-Co cells. IC50 values were calculated based on net uptake values (uptake into HEK-Co cells subtracted from the uptake into HEK-transporter-expressing cells) and the net uptake without PRA was set to 0 % uptake inhibition. Shown is mean ± SEM of at least four independent experiments.
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