Table 3. Rat Plasma Clearance,a Protein Binding,b and Stabilityc for Compounds 3−22.
rat in vivo |
rat microsomal incubation |
|||
---|---|---|---|---|
compd | Clp (mL/min/kg) | plasma Fu (%) | T1/2 (min) | Fu (%) |
3 | 12 | ND | 3 | NDd |
7 | 14 | 0.1 | 1 | 20 |
14 | 28 | 0.4 | 5 | 20 |
15 | 110 | 6.8 | ND | ND |
21 | 52 | 3.2 | ND | ND |
22 | 20 | 1.0 | ND | ND |
Plasma clearance (Clp) calculated following 1 mg/kg iv dose.
Protein binding assessed using human plasma (200 μL) or microsomal proteins (0.2 mg/mL) and test compound (1 μM).
Microsomal stability assessed using liver microsomes (0.2 mg protein/mL) and test compound (1 μM).
Not determined.