MDL28170 is a potent, selective inhibitor of calpain and cathepsin B (Ki values are 10 and 25 nM respectively) that does not inhibit trypsin-like serine proteases. MDL28170 rapidly penetrates the blood-brain barrier following systemic administration and displays neuroprotective effects in vivo.
MDL-28170 (Calpain Inhibitor III) is a potent, selective and membrane-permeable cysteine protease inhibitor of calpain. The newly-developed calpain inhibitor, MDL 28170 penetrates the blood-brain barrier and inhibits brain cysteine protease activity after systemic administration. The calpain inhibitor, MDL 28170 (50 mg/kg), was initiated at 0.5 and 3 h of recirculation following 5min of global ischemia. The calpain inhibitor, MDL 28170, protects against cortical neuronal damage even if the treatment is delayed until 3 h after reperfusion[3]. The calpain inhibitor, MDL28170, significantly improved the recovery of synaptic responses in hippocampal slices following prolonged, moderate hypoxia without hypoxic depolarization[4]. MDL28170 increased VSC4.1 motor neurons' viability under tunicamycin (an endoplasmic reticulum stress) induced injury. In a traumatic SCI (spinal cord injury) rat model, MDL28170-loaded PCL (polycaprolactone) film reduced the area of lesion cavity, and promoted recovery of locomotor behavior. Moreover, the expression of GAP-43 was upregulated after MDL28170-loaded PCL film treatment[5]. MDL-28170 (30 mg/kg, i.p.) reduces the functional and structural deterioration of corpus callosum following fluid percussion injury[6]. 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[7].
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