Table 5. Pharmacokinetic Parameters of Compound 10.
Mouse |
Rat |
Dog |
||||
---|---|---|---|---|---|---|
PK Parameters | IV dose | PO dose | IV dose | PO dose | IV dose | PO dose |
Dose (mg/kg) | 2 | 10 | 0.5 | 5 | 1 | 2 |
Cl (mL/min/kg) | 54 | 156 | 61 | |||
Vss (L/kg) | 3.9 | 37 | 1.5 | |||
AUCN (μM·h) | 1.38 | 0.118 | 0.188 | 0.61 | ||
T1/2 (h) | 5.2 | 5.5 | 2.3 | |||
Cmax (μM) | 0.48 | 0.050 | 0.071 | |||
Tmax (h) | 0.25 | 0.38 | 0.75 | |||
F (%) | 18 | 16 | 7.2 | |||
Plasma protein binding % | 96.2 | 88.6 | 91.2 |
Plasma protein binding % in human plasma is 91.5.