MDL-28170

MDL-28170 (Calpain Inhibitor III) is a potent, selective and membrane-permeable cysteine protease inhibitor of calpain that rapidly penetrates the blood-brain barrier following systemic administration^[1][2]. MDL-28170 also block γ-secretase^[4]. IC50 & Target: Calpain^[1]. In Vitro: MDL-28170 significantly and time-dependently improves the recovery of synaptic responses in hippocampal slices following prolonged, moderate hypoxia without hypoxic depolarization^[1].
MDL-28170 dose-dependently inhibits brain cysteine proteinase activity (in vitro K_i= 0.01 μM)^[2]. In Vivo: Treatment with MDL-28170 (50 mg/kg, i.p.) completely prevents the striatal damage in four animals in each of the two treatment groups. The numbers of necrotic neurons are reduced by 85% and 68% in animals in which MDL-28170 injections are initiated at 0.5 and 3 h of recirculation, respectively^[2].
MDL-28170 (30 mg/kg, i.p.) reduces the functional and structural deterioration of corpus callosum following fluid percussion injury^[3].
MDL-28170 (10 mg/kg, i.p.) significantly improves nerve function parameters in diabetic rats. MDL-28170 (3 and 10 mg/kg, i.p.) improves nociceptive behavior in diabetic rats^[5].