Table 3. In Vitro–in Vivo Profilea of (−)-17.
solubility (μM) | 100 |
Caco-2 Papp (10–6 cm/s), efflux ratio | 5.8, 0.4 |
human hepatocytes T1/2 (min) | >173 |
hERG, Nav1.5, IKs, Kv4.3 Cav3.2, Cav1.2 IC50 (μM) | >33 |
reactive metabolite formation | no (0.0) |
cytochrome P450 IC50 (μM) | >20 |
pharmacokinetics | C57Bl/6J mouse |
plasma protein binding Fu (%) | 5 |
dose iv/po (μmol/kg) | 10/50 |
CLu (mL/min/kg) | 306 |
F (%) | 95 |
Vss (L/kg) | 0.52 |
Please see the Supporting Information for experimental details.