TABLE 1.
In vitro and in vivo pharmacokinetic properties of VU0071063
| Parameter | Value |
|---|---|
| VU0071063 | |
| Molecular weight | 326 |
| cLogP | 2.64 |
| In vitro pharmacokinetics | |
| Rat fu plasma | 0.048 |
| Mouse fu plasma | 0.133 |
| Rat fu brain | 0.023 |
| Mouse fu brain | 0.024 |
| Rat CLHEP (ml/min per kilogram) | 49.6 |
| Mouse CLHEP (ml/min per kilogram) | 73.2 |
| Mouse and rat plasma brain levels | |
| Rat Kp | 8.06 |
| Rat Kp,uu | 3.86 |
| Mouse Kp | 2.22 |
| Mouse Kp,uu | 0.4 |
| In vivo pharmacokinetics (mouse, IP, 30 mg/kg) | |
| Tmax | 0.25 h |
| Cmax | 6.8 μM |
| AUC(0–4 h) | 11.4 μM*h |
CLHEP, predicted hepatic clearance; Kp - ratio of total plasma AUC to total Brain AUC; Kp,uu -ratio of unbound plasma AUC to unbound Brain AUC; Cmax, maximal plasma concentration.