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A potent and selective cell permeable calpain inhibitor. Inhibits oxidative damage-induced apoptosis in PC12 cells and capsaicin-induced apoptosis in dorsal root ganglion neurons. It protects against anoxia in rat optic nerves and reduces neuronal damage in an animal model of global cerebral ischemia(50 mg/kg). In isolated hippocampal pyramidal neurons, it inhibits Ca²⁺-induced suppression of neurite outgrowth (complete inhibition at 20 µM). Calpain I Ki = 8 nM; Cathepsin B Ki = 24 nM in isolated enzyme assays. IC50 = 0.3 µM in intact cell assay.
- Calpain and cathepsin inhibitor
Soluble in DMSO (200 mM).
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