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. 2022 Mar 2;11:e72468. doi: 10.7554/eLife.72468

Table 1. Potency and isoform selectivity of NBI-921352 for human and mouse NaV channels.

Note that IC50s for the neuronal sodium channels, NaV 1.1, NaV 1.2, and NaV1.6, have been more accurately defined than those for non-neuronal sodium channels. Explicit IC50’s for NaV1.3, NaV1.4, and NaV1.5 were not determined since the inhibition at the highest concentration tested (30 µM) was <50%. IC50’s are the mean of 3 separate biological replicates of the IC50 determinations for each channel. The error is shown as the 95% confidence interval of the mean IC50. None of the other tested isoforms displayed IC50’s within the 95% confidence interval of the NaV1.6 IC50 and the confidence intervals were well separated as well.

NaV1.6 NaV1.1 NaV1.2 NaV1.3 NaV1.4 NaV1.5 NaV1.7
Human IC50 (µM) 0.051 39 6.9 > 30 > 30 > 30 14
95% CI 0.030–0.073 31–47 1.6–12 - - - 6.4–22
Human Selectivity hNaV1.X / hNaV1.6 1 756 134 > 583 > 583 > 583 276
Mouse IC50 (µM) 0.058 41 11
Mouse Selectivity mNaV1.X / mNaV1.6 1 709 191