Transporter | Probe Substrate | IC50 |
---|---|---|
µM | ||
OATP1B1 | Pitavastatin (0.1 µM) | 18.0 ± 2.4 |
OATP1B3 | Bromosulfophthalein (BSP) (0.1 µM) | 4.9 ± 1.3 |
OATP2B1 | Estrone-3-sulfate (0.1 µM) | >50 |
Pgp | Digoxin (0.1 µM) | >300 |
BCRP | Methotrexate (10 µM) | 81 ± 28 |
MRP2 | Ethacrynic acid glutathione (EA-SG) (2 µM) | >100 |
BCRP, breast cancer resistance protein; MRP2, multidrug resistance protein 2; OATP, organic anion-transporting polypeptide; Pgp, P-glycoprotein.