In vitro evaluation of EPAC and its metabolites as a potential perpetrator for OAT1-, OAT3 or OCT2-mediated drug-drug interactions
| Compound | Free Cmax | OAT1 | OAT3 | OCT2 | |||
|---|---|---|---|---|---|---|---|
| IC50 | Cmax/IC50 | IC50 | Cmax/IC50 | IC50 | Cmax/IC50 | ||
| μM | μM | μM | μM | ||||
| EPAC | 0.049 | >300 | <0.0002 | 21 | 0.002 | 203 | 0.0002 |
| M9 | 1.95 | N/I | N/A | >300 | <0.007 | N/I | N/A |
| M11 | 0.263 | N/I | N/A | 14 | 0.019 | 23 | 0.011 |
| M12 | 0.080 | 8.6 | 0.009 | 21 | 0.004 | 21 | 0.004 |
N/A, Not applicable; N/I, No inhibition was observed over the range of the concentrations tested.