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MDL-28170

Calpain and cathepsin inhibitor
 
BML-PI130-0010 10 mg 64.00 USD
 
BML-PI130-0050 50 mg 248.00 USD
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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.

Product Specification

Alternative Name:N-Benzyloxycarbonylvalylphenylalaninal
 
Sequence:Z-Val-Phe-CHO
 
Formula:C22H26N2O4
 
MW:382.5
 
CAS:88191-84-8
 
Purity:≥98% (HPLC)
 
Appearance:White solid.
 
Solubility:Soluble in DMSO (200mM).
 
Shipping:Shipped on Blue Ice
 
Long Term Storage:-20°C
 
BML-PI130 structure
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BML-PI130 structure

Product Literature References

Calpain inhibitors confer biochemical, but not electrophysiological, protection against anoxia in rat optic nerves: Q. Jiang et al.; J. Neurochem. 74, 2101 (2000), Abstract;
Oxidative stress and Ca2+ influx upregulate calpain and induce apoptosis in PC12 cells: S.K. Ray et al.; Brain Res. 852, 326 (2000), Abstract;
D-amino acid containing, high-affinity inhibitors of recombinant human calpain I: S. Chatterjee et al.; J. Med. Chem. 41, 2663 (1998), Abstract;
Postischemic treatment with calpain inhibitor MDL 28170 ameliorates brain damage in a gerbil model of global ischemia: P.A. Li et al.; Neurosci. Lett. 247, 17 (1998), Abstract;
Capsaicin-induced neurotoxicity in cultured dorsal root ganglion neurons: involvement of calcium-activated proteases: P.S. Chard et al.; Neuroscience 65, 1099 (1995), Abstract;
Calpain inhibitors block Ca(2+)-induced suppression of neurite outgrowth in isolated hippocampal pyramidal neurons.: D.K. Song et al.; J. Neurosci. Res. 39, 474 (1994), Abstract;

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For Research Use Only. Not for use in diagnostic procedures.
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