Name | NaV1.7 inhibitor 51 |
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Description | NaV1.7 inhibitor 51 is a highly potent, selective, orally active NaV1.7 inhibitor with IC50 of 10.7 nM in FLIPR membrane potential assay, no significant activity against NaV1.5 (IC50>10 uM).NaV1.7 inhibitor 51 shows good selectivity against other NaV isoforms and minimal inhibition at 10 uM for the resting state across different NaV isoforms.NaV1.7 inhibitor 51 exhibits state-dependent block of human, monkey, and mouse NaV1.7 with a similar potency range.NaV1.7 inhibitor 51 shows significant effects on the CCI-induced neuropathic pain model. |
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References | 1. Vidya Ramdas, et al. J Med Chem. 2020 Jun 11;63(11):6107-6133. |
Molecular Formula | C24H20F3N5O2S |
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Molecular Weight | 499.512 |