Figure 4.
Glyburide and glipizide uptake in HEK-293 Flp-ln cells recombinantly expressing SLCO1B1 or SLCO1B3. A: Uptake of [3H]-glyburide and [3H]-glipizide in HEK-293 Flp-ln stable cells expressing EV, SLCO1B1, or SLCO1B3. Rifampicin (50 μmol/L) is used as a canonical inhibitor of SLCO1B1 and SLCO1B3 P values, representing significance from EV, were determined by one-way ANOVA followed by Dunnett two-tailed test. ****P < 0.0001; ***P < 0.001; **P < 0.01; *P < 0.05. Bars represent the mean ± SEM uptake from three wells. Values shown are from a representative experiment of at least three independent studies. B: Uptake of [3H]-estrone sulfate, [3H]- glyburide, and [3H]-glipizide in HEK-293 Flp-ln stable cells expressing EV, SLCO1B1, and SLCO1B1 V174A. Estrone sulfate is a canonical substrate of SLCO1B1 and is used as a positive control in this assay. P values, for significance from EV, were determined by one-way ANOVA followed by Dunnett two-tailed test. ****P < 0.0001; ***P < 0.001; **P < 0.01; *P < 0.05. Bars represent the mean ± SEM uptake from four wells from a representative experiment. The uptake values for [3H]-glyburide and [3H]-glipizide shown are from at least four independent studies with three or four replicates per study. C: Inhibition of [3H]-glyburide uptake by atorvastatin and simvastatin acid in HEK-293 Flp-ln stable cells expressing SLCO1B1 and SLCO1B3. Each point represents the mean ± SEM uptake from four wells. Values shown are from a representative experiment of two independent studies.