Size: | Price | Quantity | |
---|---|---|---|
5 mg | $40.00 | ||
25 mg | $160.00 |
MDL-28170 (88191-84-8) is 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.1 It penetrates the blood-brain barrier and inhibits brain cysteine protease activity after systemic administration, ameliorating brain damage in a gerbil model of global ischemia.2 Displays neuroprotective effects in neurotrauma rodent models.3 Calpain I Ki = 8 nM; Cathepsin B Ki = 24 nM in isolated enzyme assays. IC50 = 0.3 µM in intact cell assay.4
References/Citations:
1) Chard et al. (1995), Capsaicin-induced neurotoxicity in cultured dorsal root ganglion neurons: involvement of calcium-activated proteases; Neuroscience, 65 1099
2) Li et al. (1998), Postischemic treatment with calpain inhibitor MDL28170 ameliorates brain damage in a gerbil model of global ischemia; Neurosci. Lett., 247 17
3) Thompson et al. (2010), A pharmacological analysis of the neuroprotective efficacy of the brain- and cell-permeable calpain inhibitor MDL-28170 in the mouse controlled cortical impact traumatic brain injury model; J. Neurotrauma, 27 2233
4) Chatterjee et al. (1998), D-amino acid containing, high-affinity inhibitors of recombinant human calpain I; J. Med. Chem., 41 2663
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MDL-28170 (88191-84-8) is 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.1 It penetrates the blood-brain barrier and inhibits brain cysteine protease activity after systemic administration, ameliorating brain damage in a gerbil model of global ischemia.2 Displays neuroprotective effects in neurotrauma rodent models.3 Calpain I Ki = 8 nM; Cathepsin B Ki = 24 nM in isolated enzyme assays. IC50 = 0.3 µM in intact cell assay.4
References/Citations:
1) Chard et al. (1995), Capsaicin-induced neurotoxicity in cultured dorsal root ganglion neurons: involvement of calcium-activated proteases; Neuroscience, 65 1099
2) Li et al. (1998), Postischemic treatment with calpain inhibitor MDL28170 ameliorates brain damage in a gerbil model of global ischemia; Neurosci. Lett., 247 17
3) Thompson et al. (2010), A pharmacological analysis of the neuroprotective efficacy of the brain- and cell-permeable calpain inhibitor MDL-28170 in the mouse controlled cortical impact traumatic brain injury model; J. Neurotrauma, 27 2233
4) Chatterjee et al. (1998), D-amino acid containing, high-affinity inhibitors of recombinant human calpain I; J. Med. Chem., 41 2663
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