Compound | I1 (μM) | I2 (μM) | P-gp | BCRP | ||||
---|---|---|---|---|---|---|---|---|
IC50 | I1/ IC50 | I2/ IC50 | IC50 | I1/ IC50 | I2/ IC50 | |||
μM | μM | |||||||
EPAC | 1.57 | 2740 | >500 | <0.004 | <5.5 | N/I | N/A | N/A |
M9 | 10.2 | Unknown | N/I | N/A | N/A | N/I | N/A | N/A |
M11 | 2.10 | Unknown | N/I | N/A | N/A | >300 | <0.007 | N/A |
M12 | 2.10 | Unknown | N/I | N/A | N/A | 32 | 0.066 | N/A |
I1, Mean steady-state total Cmax after 300-mg twice daily dose; I2, 300-mg (0.685 mmol) dose divided by 250 ml;
N/A, not applicable; N/I, no inhibition was observed over the range of the concentrations tested.