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).