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. 2018 Jun 23;9(7):600–605. doi: 10.1021/acsmedchemlett.7b00507

Table 3. In Vitroin 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
a

Please see the Supporting Information for experimental details.