DS-1971a is a potent, selective, and orally active NaV1.7 inhibitor, with IC50s of 22.8 and 59.4 nM for hNaV1.7 and mNaV1.7, respectively. DS-1971a exerts analgesic effects[1]
DS-1971a exhibits a favorable toxicological profile[1]
DS-1971a (0.1-1 mg/kg; p.o.) shows mitigated thermal hyperalgesia in a dose-dependent manner in partial sciatic nerve ligation (PSL) mice[1]
Reference:
[1]. Shinozuka T, et al. Discovery of DS-1971a, a Potent, Selective NaV1.7 Inhibitor [published online ahead of print, 2020 May 26]. J Med Chem. 2020;10.1021/acs.jmedchem.0c00259.