TABLE 2

IC50 values for the inhibitory effects of typical substrates of OATP-B on uptake of [3H]estrone-3-sulfate by HEK293/OATP-B and Caco-2 cells


Compounds

IC50*
HEK293/OATP-B
Caco-2
BSP 0.282 ± 0.062 μM 2.89 ± 0.74 μM
DHEAS 8.60 ± 0.37 μM 12.0 ± 3.4 μM
Pravastatin 1.02 ± 0.10 mM 1.06 ± 0.11 mM
Benzylpenicillin
16.0 ± 3.4 mM
10.2 ± 1.6 mM
  • * Data represent the mean ± S.E.M. (n = 3).