Table 4. PK Data for Representative Compounds.
mice IV 1 mg/kg |
mice PO 5 mg/kg |
|||||||||
---|---|---|---|---|---|---|---|---|---|---|
Cmpd # | BCATm pIC50 | BCATc pIC50 | hCell pIC50 | Clb (mL/min/kg) | t1/2 (h) | Vss (L/kg) | AUC0-inf (ng·h/mL) | Cmax (ng/mL) | F% | mice PPB (%) |
1 | 6.6 | 5.9 | 7.2 | 23 | 1.4 | 1.3 | 338 | 129 | 10 | 99.5 |
8b | 7.3 | 5.4 | 7.0 | 4.0 | 3.7 | 0.9 | 5809 | 1648 | 28 | 97.1 |