Table 3.
Pharmacokinetic profile of 21b and metabolite 21c in mice.
| PK parameter |
21b at 60 mg/kg p.o.a |
|
|---|---|---|
| 21bb | 21cc | |
| t1/2 (h) | 5.1 ± 0.4 | 6.2 ± 0.6 |
| Tmax (h) | 8.0 | 4.0 |
| Cmax (μmol/L) | 0.47 ± 0.04 | 0.29 ± 0.03 |
| AUC0−24 (μmol·h/L) | 5.0 ± 0.41 | 3.3 ± 0.16 |
| AUC0−∞ (μmol·h/L) | 5.4 ± 0.47 | 3.6 ± 0.18 |
a
Prodrug 21b was dosed via a single p.o. route at indicated concentrations.
b
PK parameters of the parent 21b.
c
PK parameters of the metabolite 21c. All data are mean ± SD, n = 5. Additional data are shown in the Supporting Information Fig. S9 and Table S3.