HEK293 OATP-overexpressing cell line | Vmax,cells (pmol substrate/min per milligram protein) |
TG | 3.89 | 42.72 |
AG | 44.05 | 237.5 |
EtioG | 2.32 | 15.84 |
DHTG | 1.21 | 3.08 |
Km, cells (µM) |
TG | 56.71 | 110.4 |
AG | 46.18 | 29.27 |
EtioG | 6.16 | 19.81 |
DHTG | 71.27 | 69.57 |
Transporter abundance (Ecell, pmol transporter/mg protein) | 6.86 | 7.42 |
Clearance (CLint,cell, µl/min per picomole transporter) = Vmax,cell/Km,cell/Ecell |
TG | 0.01 | 0.05 |
AG | 0.14 | 1.09 |
EtioG | 0.05 | 0.11 |
DHTG | 0.002 | 0.01 |
Fractional contribution of individual transporter (ft) | OATP1B1 | OATP1B3 |
TG | 0.16 | 0.84 |
AG | 0.11 | 0.89 |
EtioG | 0.34 | 0.66 |
DHTG | 0.29 | 0.71 |
Liver | Transporter abundance (Eliver, pmol transporter/mg protein) | 3.64 | 1.49 |
TM-PPGT (mg protein/gram of tissue) | 49.40 | 49.40 |
Tissue weight (kg) | 1.60 | 1.60 |
Estimated hepatic clearance (CLint, µl/min) = Clint,cell * Eliver, total |
TG | 2875 | 6142 |
AG | 39,976 | 128,786 |
EtioG | 15,742 | 12,691 |
DHTG | 714 | 703 |
Fractional contribution of individual transporter (ft) | | |
TG | 0.32 | 0.68 |
AG | 0.24 | 0.76 |
EtioG | 0.55 | 0.45 |
DHTG | 0.50 | 0.50 |