Figure 1

Inhibitory effects of raloxifene species on active uptake of estrone-3-sulfate into CHO cells expressing OATP1B1 or OATP1B3. Raloxifene-6-β-glucuronide (M1), raloxifene-4'- β -glucuronide (M2), raloxifene-6,4'-diglucuronide (M3), indocyanine green (ICG), estrone-3-sulfate (E-3-S).E-3-S was used at concentration 0.5 μM, and cells were incubated with substrate and inhibitor for 5 minutes. The results are shown as percentage of control uptake measured in the absence of inhibitor. Each column represents the mean ± SD (n = 4) and (*) indicates a significant difference from the control (p < 0.05).