MDL-28170 | Calpain inhibitor
NMR (Conforms)
Available Options
| 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
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
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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