Table 4. PK Parameters for Compounds 5f, 5g, and 6.
| compound | routea | dose (mg/kg) | Cmax (nM) | AUC (nM·h) | %F | %HBF | Vss (L/kg) |
|---|---|---|---|---|---|---|---|
| 5f | iv (r) | 0.5 | >100 | 3.2 | |||
| 5f | po (r) | 3.0 | 752 | 666 | 92 | ||
| 5g | iv (r) | 0.5 | >100 | 1.1 | |||
| 5g | po (r) | 3.0 | 992 | 1150 | 100 | ||
| 5g | iv (c) | 0.5 | 70 | 3.5 | |||
| 5g | po (c) | 2.0 | 138 | 739 | 100 | ||
| 6 | iv (r) | 0.5 | 96 | 2.0 | |||
| 6 | po (r) | 3.0 | 562 | 1134 | 59 | ||
| 6 | iv (c) | 0.3 | 48 | 1.2 | |||
| 6b | po (c) | 2.0 | 56 | 388 | 12 |
r = rat, c = cyno.
Adjusted from 1 mg/kg dose for comparison.