NA-184 is a potent, selective calpain-2 inhibitor with Ki of 50 nM (human calpain-2) and IC50 of 134 nM (mouse calpain-2).
NA-184 displays 20-fold selective over mouse calpain-1 (IC50=2826 nM).
NA-184 does not exhibit significant inhibition on a variety of other cysteine-, serine- or metallo-proteases at concentrations up to 10 μM, with exception of cathepsin L and B (Ki=1.9 and 220 nM).
NA-184 inhibits TBI-induced calpain-2 activation and cell death in mice and rats, both male and females.
NA-184 exhibites properties, including stability in plasma and liver and blood–brain barrier permeability.
