Table 4. Cellular Potencya and Rat Pharmacokinetic Profileb for Selected Piperidine-Ether Compounds.
compd | MK-5172 | 21 | 23 | 24 | 25 | 35 | 37 |
---|---|---|---|---|---|---|---|
1b EC50, nM | 1.5 | 0.25 | 0.21 | 0.53 | 0.73 | 0.48 | 0.62 |
3a EC50, nM | 13.0 | 3.1 | 7.8 | 5.2 | 13.5 | 1.06 | 0.26 |
rat AUC, μM·h | 0.7 | 2.7 | 0.01 | 2.3 | 2.8 | 0.01 | 1.2 |
Cell-based replicon assays conducted in presence of 10% fetal-bovine serum (FBS); EC50 determination was conducted using a TaqMan-based assay.
5 mg/kg, po, methyl cellulose (PEG400 for MK5172).