Drug intelligence / Profile preview

Chinese Academy of Sciences hNaV1.8 compound (R)-40

Development stage
Unknown
Lead developer
Chinese Academy of Sciences
01

Overview

Chinese Academy of Sciences hNaV1.8 compound (R)-40: sourced facts only. name: "Conformational restriction strategy and subsequent optimization led to the identification of the chroman derivative (R)-40 as the most promising hNaV1.8 inhibitor showing an IC50 value of 5.9 ± 1.0 nM and good selectivity over other tested NaV channels and hERG channel." [PMID:40347793]; target: "Conformational restriction strategy and subsequent optimization led to the identification of the chroman derivative (R)-40 as the most promising hNaV1.8 inhibitor showing an IC50 value of 5.9 ± 1.0 nM and good selectivity over other tested NaV channels and hERG channel." [PMID:40347793]; developer: "Department of Medicinal Chemistry, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China; State Key Laboratory of Chemical Biology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China; School of Physical Science and Technology, ShanghaiTech University, Shanghai, 201210, China; Lingang Laboratory, Shanghai, 200031, China." [PMID:40347793]; stage: "Notably, (R)-40 exerted dose-dependent analgesic activities in both rat models with postoperative and inflammatory pain, and a wide safety margin in neurotoxicity evaluation." [PMID:40347793]

02

Targets

SCN10A (Sodium channel protein type X alpha subunit)

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