Skip to main content
. 2021 Jun 1;12(6):1038–1049. doi: 10.1021/acsmedchemlett.1c00218

Table 2. Western SAR and Selectivity over Nav1.6.

graphic file with name ml1c00218_0009.jpg

graphic file with name ml1c00218_0010.jpg

a

Estimated hyperpolarized state potency as measured by Qube in HEK293 cells stably expressing human Nav1.7 or Nav1.6; IC50 values are estimated from ≥3 cellular measurements at varying compound concentrations and standard deviation <50% of average value shown.

b

Monolayer assay in MDCK cells.

c

Rat CLint = (84 × rat CL)/[rat fu × (84-rat CL)]; units mL/min/kg; IV, 0.05 mpk cassette dosing or 2 mpk single dosing in DMSO/PEG400/water (20/60/20); PO, 10 mpk in PEG400/Tween90/water (40/10/50).