Mean noncompartmental pharmacokinetics parameters for compound 1 and M1 after oral administration of compound 1 to mice
A total of 24 animals (3 per time point) were used to generate the data for each dose group.
| Dose | Cmax | Tmax | t1/2 | AUC0-inf | CL/F | Fa | |
|---|---|---|---|---|---|---|---|
| mg/kg | μM | h | h | μM⋅h | l/h⋅kg | % | |
| Compound 1 | 20 | 0.782 | 0.25 | 1.23 | 1.31 | 26.2 | 21.1 |
| 50 | 10.7 | 1.0 | 2.30 | 23.7 | 3.65 | 151 | |
| 100 | 15.2 | 1.0 | 2.17 | 37.4 | 4.63 | 120 | |
| M1 | 20 | 0.881 | 1.0 | ND | 2.99 | ND | ND |
| 50 | 2.75 | 2.0 | ND | 10.9 | ND | ND | |
| 100 | 3.27 | 4.0 | ND | 23.3 | ND | ND |
ND, not determined; Tmax is defined as the time at which the maximum concentration of drug in plasma (Cmax) is observed; Vss, volume at steady state.
↵a Relative to 2 mg/kg i.v. dose.