TABLE 1

Kinetic parameters of the uptake of compounds by transporter-expressing HEK293 cells

Data shown in Fig. 1 were used to determine these parameters calculated by nonlinear regression analysis. Each point represents the mean ± S.E. (n = 3).


Transporter

Substrate

Km

Vmax

Vmax/Km

Pdif
μM pmol/min/mg μl/min/mg μl/min/mg
OATP2 E-sul 0.458 ± 0.154 60.3 ± 8.8 132 ± 19
CCK-8 Not significantly transported
Pitavastatin 3.00 ± 0.39 230 ± 17 76.6 ± 5.6
E217βG 8.29 ± 0.42 131 ± 5 15.8 ± 0.6
OATP8 E-sul Not significantly transported
CCK-8 3.82 ± 2.20 102 ± 60 26.7 ± 15.7 11.4 ± 2.6
Pitavastatin 3.25 ± 0.44 100 ± 8 30.6 ± 2.3

E217βG
24.6 ± 7.6
56.8 ± 16.1
2.31 ± 0.65

  • Pdif, nonsaturable uptake clearance (microliters per minute per milligram of protein).