Table 3. Pharmacokinetic Profile of 3a.
| species | dose route | dose (mg/kg) | tmax (h) | Cmax (μM) | AUCb (μM·h) | CLPl (mL/min/kg) | VSS (L/kg) | t1/2 (h) | F% |
|---|---|---|---|---|---|---|---|---|---|
| mouse | IV | 5 | 13 | 13.8 | 0.6 | 1.8 | |||
| PO | 10 | 0.25 | 22.7 | 17 | 66 | ||||
| rat | IV | 4 | 9.4 | 15.3 ± 0.7 | 2.2 ± 0.5 | 3.3 | |||
| PO | 8 | 0.3 ± 0.1 | 14.9 | 32 | 100 | ||||
| dog | IV | 1 | 3.5 | 10.7 ± 2.4 | 2.1 ± 1.2 | 5.5 | |||
| PO | 2 | 0.8 ± 0.3 | 1.5 | 4.0 | 59 | ||||
| monkey | IV | 1 | 7.5 | 5.9 ± 2.7 | 3.9 ± 1.5 | 26.3 | |||
| PO | 2 | 0.9 ± 0.1 | 1.4 | 8.5 | 65 |
For each experimental study, n ≥ 3.
AUC0–8h reported here, not AUCINF.