Table 4. In Vitro ADME Data and Rat Pharmacokinetic Profilea of Selected Compounds.
| in vitro ADME |
rat PK |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| compd | h-PB (%free) | h-IntCL (L/(h kg)) | Caco2 Pm (× 10–6 cm/s) | Cmax (p.o., nM) | AUCinf (p.o., nM h) | T1/2 (h) | Vss (L/kg) | CL (L/(h kg)) | F (%) | L/Pb |
| 11 | 4.3 | 1.1 | 0.4 | 151 | 669 | 3.8 | 9.2 | 4.1 | 46 | 48 |
| 12 | 9.9 | 0.9 | 0.6 | 75 | 441 | 3.1 | 21.9 | 7.2 | 49 | 355 |
| 16 | 4.3 | 1.0 | 4.5 | 434 | 4050 | 5.7 | 7.6 | 1.1 | 85 | 30 |
a
1 mg/kg i.v. and 3 mg/kg p.o.
b
The liver/plasma ratio of compound concentration was collected at 2 h post p.o. dosing.