Expression System | OATPs Investigated | Digoxin Uptake Experiments | Positive Controls/Inhibitors/Negative Controls | ||||||
---|---|---|---|---|---|---|---|---|---|
Digoxin Concentration | Uptake Time | Temperature | Control Substrate | Uptake Time | Uptake Inhibitor | Negative Control | |||
μM | °C | ||||||||
GSK | HEK293 cells transduced with recombinant BacMam virus | OATP1B1 | 0.01, 0.05, 0.25, 0.5, 5, and 50 | 3 min | 37 | 0.02 μM E17βG | 3 min | Rifamycin | |
OATP1B3 | 10 min | 0.02 μM E17βG | 10 min | Rifamycin | |||||
OATP1A2 | 30 s | 0.02 μM E3S | 30 s | Ketoconazole | |||||
OATP2B1 | 30 s | 0.02 μM E3S | 30 s | Montelukast | |||||
BI | HEK293 and CHO cells transiently transfected with transporter containing plasmid DNA | OATP1B3 | 1 | 37 | 1 μM CCK-8 | 10 min | Rifamycin | ||
OATP2B1 | 0.5 μM EE3S | 3 min | Rifamycin | HEK293 and CHO cells transiently transfected with control DNA | |||||
Pfizer | Stably transfected HEK293 cells | OATP1B1 | 1 & 10 | 4 min | 37 | 5 μM E17βG | 4 min | Rifamycin | Untransfected HEK293 cells |
OATP1B3 | 5 μM E17βG | Rifamycin | |||||||
OATP2B1 | 5 μM UK191005 | ||||||||
Solvo | CHO cells | OATP1B1 | 1.2 & 11 | 15 min | 37 | 0.1 μM E3S | 15 min | Cerivastatin | |
CHO cells | OATP1B3 | 0.1 μM E3S | Fluvastatin | ||||||
MDCKII cells | OATP2B1 | 10 μM Fluo-3 | Fluvastatin |
E3S, estrone 3-sulfate; E17βG, estradiol-17β-d-glucuronide; CCK-8, cholecystokinin-8.