DS-1971a

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].

Signaling Pathways >> Membrane Transporter/Ion Channel >> Sodium Channel

Research Areas >> Neurological Disease

IC50: 22.8 nM (hNaV1.7), 59.4 nM (mNaV1.7)[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]. Animal Model: Male Slc:ddY mice (PSL model)[1] Dosage: 0.1, 0.3, and 1 mg/kg Administration: P.o. Result: A significant dose-dependent suppression of thermal hyperalgesiain 0.3 and 1 mg/kg administered groups. The ED50 of DS-1971a at the peak efficacy was 0.32 mg/kg.

[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.