TABLE 1.
Transporter | Substrate | Km (μM) | Vmax (nmol/mg protein × min) | Vmax/Km |
OATP1B1 | BDE47 | 0.31 ± 0.01 | 13.5 ± 1.33 | 44.0 ± 2.8 |
BDE99 | 0.91 ± 0.02 | 13.9 ± 1.70 | 15.4 ± 2.2 | |
BDE153 | 1.91 ± 0.17 | 2.4 ± 0.19 | 1.2 ± 0.02 | |
OATP1B3 | BDE47 | 0.41 ± 0.06 | 15.7 ± 1.71 | 38.0 ± 1.1 |
BDE99 | 0.70 ± 0.03 | 12.8 ± 0.76 | 18.3 ± 0.1 | |
BDE153 | 1.66 ± 0.48 | 22.6 ± 0.58 | 1.5 ± 5.3 | |
OATP2B1 | BDE47 | 0.81 ± 0.06 | 17.6 ± 1.1 | 22.6 ± 1.1 |
BDE99 | 0.87 ± 0.22 | 8.9 ± 0.9 | 10.5 ± 1.6 | |
BDE153 | 0.65 ± 0.07 | 14.6 ± 3.1 | 28.1 ± 8.1 |
Note. Transport rates at increasing concentrations were determined at 37°C in OATP-expressing and wild-type CHO or vector-transfected cells. Transport values obtained from OATP-expressing cells were corrected with values obtained from wild-type cells, and the resulting net carrier-mediated uptake values were fitted by nonlinear regression analysis to the Michaelis-Menten equation. Means ± SE are given for three to four experiments.