Table 2.
PK Parameters of the Compounds 21b,e–j in Mice by Oral Cassette Dosing at 5 mg/kg (n =1) and in Rats by Oral Administration at 1 mg/kg (n=4).
species | Inhibitors | Tmax (h) | Cmax (nM) | AUC (nM*h) | t1/2 (h) |
---|---|---|---|---|---|
Mouse | 21h | 0.8 | 190 | 375 | 2.4 |
21i | 0.8 | 260 | 980 | 2.6 | |
21j | 0.8 | 290 | 1335 | 2.4 | |
21e | 0.5 | 100 | 125 | 3.1 | |
21b | 0.5 | 19 | 35 | 1.0 | |
21g | 0.5 | 42 | 100 | 3.5 | |
21f | 0.5 | 20 | 22 | 1.7 | |
Rat | 21i | 1.5 ± 0.6 | 415 ± 139 | 2764 ± 804 | 13 ± 4 |
21j | 1.0 ± 0.7 | 180 ± 71 | 1230 ± 521 | 12 ± 6 |