Inhibitory effect of typical inhibitors on the (A) OCT1, (B) OCT2, (C) OAT1, (D) OAT3, (E) OATP1B1, and (F) OATP1B3-mediated uptake. Transporter mediated uptake of probe substrate were calculated by subtracting the uptake in HEK293-mock cells from the uptake in HEK293 cells overexpressing respective transporters. The concentrations and probe substrates were as follows: 0.1 μM [3H]methyl-4-phenylpyridinium (MPP+) for OCT1 and OCT2, 0.1 μM [3H]para-aminohippuric acid (PAH) for OAT1, 0.1 μM [3H]estrone-3-sulfate (ES) for OAT3 and OATP1B1, and 0.1 μM [3H]estradiol-17β-d-glucuronide (EG) for OATP1B3. The typical inhibitors were used as follows: TEA (0–50 mM) for OCT1 and OCT2, probenecid (0–250 μM) for OAT1 and OAT3, and rifampin (0–250 μM) for OATP1B1 and OATP1B3. Data are the mean ± SD from triplicate measurements.