MDL-28170

BML-PI130

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Calpain and cathepsin inhibitor

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 K_i= 8 nM; Cathepsin B Ki = 24 nM in isolated enzyme assays. IC50 = 0.3 µM in intact cell assay.

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Product Details

Alternative Name	N-Benzyloxycarbonylvalylphenylalaninal
Appearance	White solid.
CAS	88191-84-8
Formula	C₂₂H₂₆N₂O₄
MW	382.5
Purity	≥98% (HPLC)
Sequence	Z-Val-Phe-CHO
Solubility	Soluble in DMSO (200mM).

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended.
Long Term Storage	-20°C
Shipping	Blue Ice

Regulatory Status	RUO – Research Use Only

Oxidative stress and Ca2+ influx upregulate calpain and induce apoptosis in PC12 cells: S.K. Ray et al.; Brain Res. 852, 326 (2000), Abstract
Calpain inhibitors confer biochemical, but not electrophysiological, protection against anoxia in rat optic nerves: Q. Jiang et al.; J. Neurochem. 74, 2101 (2000), 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
D-amino acid containing, high-affinity inhibitors of recombinant human calpain I: S. Chatterjee et al.; J. Med. Chem. 41, 2663 (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