IC50 values for uptake and efflux transporter inhibition with phosphodiester or phosphorothioate oligonucleotides
| Transporter | Substrate | IC50 | |||
|---|---|---|---|---|---|
| PD-GP | PT-GP | PD-Ac | PT-Ac | ||
| μM | |||||
| OATP1B1 | Estradiol 17-β-glucuronide | >100 | 90 | >100 | >100 |
| OATP1B3 | Estradiol 17-β-glucuronide | >100 | 14 | >100 | 92 |
| OAT1 | p-Aminohippuric acid | 46 | 12 | 52 | 16 |
| OAT3 | Estrone 3-sulfate | >100 | 26 | 69 | >100 |
| OCT1 | Tetraethylammonium bromide | >100 | >100 | >100 | >100 |
| OCT2 | Metformin | 17 | 14 | 27 | 29 |
| P-gp | Digoxin | >100 | >100 | >100 | >100 |
| BCRP | Prazosin | >100 | >100 | >100 | >100 |