Figure 3.

atROL is a potent inhibitor of OATP1A2-mediated E3S uptake. (A) atROL inhibition on E3S uptake in the OATP1A2 over-expressing HEK293 cells. Uptake of 300 nM ³H-E3S was assessed in the presence or absence of 10 μM or 300 μM atROL as described in Methods. (B) IC₅₀ value of atROL inhibition on the uptake of 300 nM ³H-E3S was assessed in the absence or presence of a range of atROL (0.1 nM to 80 μM) in the OATP1A2 over-expressing HEK293 cells. (C) atROL inhibition on E3S uptake in the human primary RPE cells. Uptake of 300 nM ³H-E3S was assessed in the presence or absence of 10 μM atROL or methotrexate (MTX) or E3S. Data are from primary human RPE cell cultures isolated from four independent human donors. Values are mean ± SE (triplicate in each experiment, each experiment was repeated three times. *P < 0.05; **P < 0.01; ***P < 0.001; significantly different from uptake without inhibitors).