TABLE 1

Hepatic OATP-mediated transport of glyburide and metabolites

Uptake by HEK cells stably transfected with human OATP1B1, OATP1B3, and OATP2B1, normalized to uptake by wild-type HEK cells, are presented as uptake ratios. All data represent the mean ± SD (n = 3).

CompoundOATP1B1OATP1B3OATP2B1
Glyburide 1 µM1.9 ± 0.21.2a1.3a
Glyburide 10 µM1.2 ± 0.1
M1 1 µM26.1 ± 1.817.5 ± 2.615.2 ± 0.3
M1 10 µM46.7 ± 0.735.4 ± 3.521.4 ± 0.7
M2b 1 µM28.1 ± 0.722.2 ± 6.820.2 ± 0.3
M2b 10 µM39.1 ± 1.230.8 ± 0.824.8 ± 1.8
Propranolol 1 µMb1.1 ± 0.11.4 ± 0.11.3 ± 0.1
Rosuvastatin 1 µMb55.3 ± 1.114.2 ± 0.536.2 ± 2.9
  • a Taken from our previous work (Varma et al., 2014).

  • b Propranolol served as negative control and rosuvastatin served as positive control for all three OATPs.