TABLE 3

Renal OATs mediated transport of glyburide and metabolites

Uptake by HEK cells stably transfected with human OAT1 and OAT3, normalized to uptake by wild-type HEK cells, are presented as uptake ratios. All data represent the mean ± SD (n = 3).

CompoundOAT1OAT3
Glyburide 1 µM1.24 ± 0.161.25 ± 0.10
Glyburide 10 µM1.25 ± 0.090.97 ± 0.07
M1 1 µM1.48 ± 0.206.22 ± 0.04
M1 10 µM0.37 ± 0.0211.50 ± 0.86
M2b 1 µM0.64 ± 0.069.25 ± 0.54
M2b 10 µM0.96 ± 0.6313.51 ± 0.72
3H-para-aminohippuric acid (hOAT1)a74.13 ± 5.69
3H-estrone sulfate (hOAT3)a95.04 ± 1.98
  • hOAT, human OAT.

  • a Probe substrate used as positive control for the respective transporter.