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Na v channel compound profile assessed on the Qube or Qpatch*. Ten-point titrations in the Qube automated patch-clamp assay determined MSD199 to be a potent and selective compound (IC 50 = 4.7 ± 0.8 nM, mean ± SD). MSD199 potency was too weak to calculate for all other Na v isoforms except Na v 1.4, which was 1781-fold shifted to 8370 nM mean IC 50 ± 1429.

Journal: Pain

Article Title: Analgesia and peripheral c-fiber modulation by selective Na v 1.8 inhibition in rhesus

doi: 10.1097/j.pain.0000000000003404

Figure Lengend Snippet: Na v channel compound profile assessed on the Qube or Qpatch*. Ten-point titrations in the Qube automated patch-clamp assay determined MSD199 to be a potent and selective compound (IC 50 = 4.7 ± 0.8 nM, mean ± SD). MSD199 potency was too weak to calculate for all other Na v isoforms except Na v 1.4, which was 1781-fold shifted to 8370 nM mean IC 50 ± 1429.

Article Snippet: We characterized the potent, selective Na v 1.8 inhibitor 2-(4,4-difluoroazepan-1-yl)-6-methyl-N-(2-sulfamoylpyridin-4-yl)nicotinamide (C 18 H 22 N 5 O 3 S Cl, MSD199, Fig. ) using the automated patch-clamp platforms Qube or Qpatch (Sophion Bioscience A/S).

Techniques: Patch Clamp

Na v channel compound profile assessed on the Qube or Qpatch*. Ten-point titrations in the Qube automated patch-clamp assay determined MSD199 to be a potent and selective compound (IC 50 = 4.7 ± 0.8 nM, mean ± SD). MSD199 potency was too weak to calculate for all other Na v isoforms except Na v 1.4, which was 1781-fold shifted to 8370 nM mean IC 50 ± 1429.

Journal: Pain

Article Title: Analgesia and peripheral c-fiber modulation by selective Na v 1.8 inhibition in rhesus

doi: 10.1097/j.pain.0000000000003404

Figure Lengend Snippet: Na v channel compound profile assessed on the Qube or Qpatch*. Ten-point titrations in the Qube automated patch-clamp assay determined MSD199 to be a potent and selective compound (IC 50 = 4.7 ± 0.8 nM, mean ± SD). MSD199 potency was too weak to calculate for all other Na v isoforms except Na v 1.4, which was 1781-fold shifted to 8370 nM mean IC 50 ± 1429.

Article Snippet: Qube voltage-clamp experiments were performed using human embryonic kidney (HEK) 293 cell lines or Chinese Hamster Ovary cell lines stably expressing either human Na v 1.1, Na v 1.2, Na v 1.3, Na v 1.4, Na v 1.5, Na v 1.6, Na v 1.7, Na v 1.8, or Na v 1.9 on the Qube or Qpatch automated patch-clamp platforms (Sophion Bioscience A/S, Ballerup, Denmark).

Techniques: Patch Clamp