In vitro evaluation of EPAC and its metabolites as an inhibitor of efflux transporters P-gp, BCRP, and uptake transporters OATP1B1, OATP1B3, OAT1, OAT3, and OCT2
| Compound | IC50 (μM) | ||||||
|---|---|---|---|---|---|---|---|
| P-gp | BCRP | OATP1B1 | OATP1B3 | OAT1 | OAT3 | OCT2 | |
| EPAC | >500 | N/I | 59 | 51 | >300 | 21 | 203 |
| M9 | N/I | N/I | 262 | 27 | N/I | >300 | N/I |
| M11 | N/I | >300 | 68 | 19 | N/I | 14 | 23 |
| M12 | N/I | 32 | 49 | 228 | 8.6 | 21 | 21 |
N/I, No inhibition was observed over the range of the concentrations tested.