Table 4. Pharmacokinetic and Select In Vitro ADME Parameters of Compounds 2 and 43.
| Cpd 2 | Cpd 43 | |
|---|---|---|
| Mouse PK | ||
| IV dose (mg/kg) | 0.94 | 0.81 |
| AUC (ng·h/mL) | 93 | 1263 |
| Cl (mL/min/kg) | 176 | 13.1 |
| Vss (L/kg) | 6.3 | 1.6 |
| t1/2 (h) | 0.6 | 5.2 |
| oral dose (mg/kg) | 2.79 | 2.42 |
| AUC (ng·h/mL) | 42 | 2058 |
| F (%) | 12 | 54 |
| Rat PK | ||
| IV dose (mg/kg) | 0.89 | 0.83 |
| AUC (ng·h/mL) | 229 | 1288 |
| Cl (mL/min/kg) | 68 | 11 |
| Vss (L/kg) | 29.5 | 2.0 |
| t1/2 (h) | 9.0 | 3.1 |
| oral dose (mg/kg) | 2.73 | 2.55 |
| AUC (ng·h/mL) | 227 | 2261 |
| F (%) | 25 | 58 |
| Microsomal Stability | ||
| mouse t1/2 (min) | 18.2 | 65.2 |
| rat t1/2 (min) | 41.0 | 148 |