Inhibition of OATP probe substrates by digoxin
| Company | IC50 | Substrates | ||||||
|---|---|---|---|---|---|---|---|---|
| OATP1A2 | OATP1B1 | OATP1B3 | OATP2B1 | OATP1A2 | OATP1B1 | OATP1B3 | OATP2B1 | |
| μM | ||||||||
| BI | N.D. | N.D. | 54 | ∼300 | CCK-8 | E3S | ||
| GSK | 33%a | 47 | 69 | >300 | E3S | E17βG | CCK-8 | E3S |
| Solvo | N.D. | 52%a | 8.1 | 48%a | E3S | Fluo-3 | E3S | |
N.D., not determined; E3S, [3H]estrone 3-sulfate; E17βG, [3H]estradiol-17β-glucuronide; CCK-8, [3H]cholecystokinin-8.
↵a Inhibition was observed at 300 μM digoxin, but the IC50 value could not be determined.