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    Calpeptin
    Calpeptin

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    This product is for research use only, not for human use. We do not sell to patients.
    Number: - + Pieces(InventoryPieces)
    InvivoChem Cat #: V0706
    CAS #: 117591-20-5Purity ≥98%

    Description: Calpeptin (sequence: Z-Leu-nLeu-H) is a novel, potent, cell-permeable calpain inhibitor with anti-fibrotic activity. It inhibits Calpain I (porcine erythrocytes), Calpain II (porcine kidney), Papainb, and Calpain I (human platelets) with IC50s of 52 nM, 34 nM, 138 nM, and 40 nM, respectively. It attenuates apoptosis and inflammation, cell death, and axonal damage in animal model of multiple sclerosis. Calpeptin also reduced both angiopoietin-1-dependent migration and IL-6-dependent proliferation of the cells, which could be the underlying mechanism of the preventive effect of Calpeptin on pulmonary fibrosis. 

    References: Biochem Biophys Res Commun. 1988;153(3):1201-8; Am J Physiol Heart Circ Physiol. 2008;295(1):H314-26.

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    Molecular Weight (MW)362.46
    FormulaC20H30N2O4
    CAS No.117591-20-5
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 72 mg/mL (198.6 mM)
    Water: <1 mg/mL
    Ethanol: 72 mg/mL (198.6 mM)
    SMILESO=C(OCC1=CC=CC=C1)N[[email protected]](C(N[[email protected]](C=O)CCCC)=O)CC(C)C
    SynonymsCalpain; Benzylcarbonyl-leu-nleu-H; N-Cbz-leu-nleu-al. 

    Chemical Name: benzyl ((S)-4-methyl-1-oxo-1-(((S)-1-oxohexan-2-yl)amino)pentan-2-yl)carbamate

    InChi Key: PGGUOGKHUUUWAF-ROUUACIJSA-N

    InChi Code: InChI=1S/C20H30N2O4/c1-4-5-11-17(13-23)21-19(24)18(12-15(2)3)22-20(25)26-14-16-9-7-6-8-10-16/h6-10,13,15,17-18H,4-5,11-12,14H2,1-3H3,(H,21,24)(H,22,25)/t17-,18-/m0/s1


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    In Vitro

    In vitro activity: Calpeptin inhibits 20K phosphorylation in a dose-related manner in platelets stimulated by thrombin, ionomycin or collagen. In differentiating PC12 cells, Calpeptin promotes neurite elongation via inhibition of Calpain activity. In rat retinal ganglion cells, Calpeptin attenuates apoptosis, maintains normal whole-cell membrane potential, and thus provides functional neuroprotection


    Kinase Assay: Calpeptin is a potent, cell penetrating calpain inhibitor, with an ID50 of 40 nM for Calpain I in human platelets


    Cell Assay: Calpeptin reduced production of TGF-b1, IL-6, angiopoietin-1 and collagen synthesis from lung fibroblasts. Calpeptin also reduced both angiopoietin-1-dependent migration and IL-6-dependent proliferation of the cells, which could be the underlying mechanism of the preventive effect of Calpeptin on pulmonary fibrosis.

    In VivoIn a feline right ventricular (RV) PO (RVPO) model, calpeptin (0.6 mg/kg, i.v.) blocks the activation of calpain and caspase-3, cleavage of their substrates, and cardiomyocyte programmed cell death. In a rat focal cerebral ischemia–reperfusion injury model, Calpeptin reduces the neuronal apoptosis in hippocampal CA1 sector via inhibition of the expression of Caspase-3.
    Animal modelFeline right ventricular (RV) PO (RVPO) model
    Formulation & DosageDissolved in 1% DMSO in saline; 0.6 mg/kg; i.v. injection
    References

    Biochem Biophys Res Commun. 1988 Jun 30;153(3):1201-8; Am J Physiol Heart Circ Physiol. 2008 Jul;295(1):H314-26; Mol Biol Rep. 2011 Feb;38(2):905-12.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

     
    Calpeptin
    Calpain activation in cardiomyocytes of pressure-overloaded (PO) myocardium. Am J Physiol Heart Circ Physiol. 2008 Jul;295(1):H314-26.
     
    Calpeptin
    Programmed cell death of cardiomyocytes in PO myocardium. Am J Physiol Heart Circ Physiol. 2008 Jul;295(1):H314-26.
     
    Calpeptin
    Effect of in vivo administration of N-benzoylcarbonyl-Val-Ala-Asp-fluoromethylketone (Z-VD-fmk) on caspase-3-, calpain-, TUNEL-, and gelsolin-associated changes in PO myocardium. Am J Physiol Heart Circ Physiol. 2008 Jul;295(1):H314-26.
     
    Calpeptin
    Enrichment of gelsolin in calpain and TUNEL-positive cardiomyocytes of PO myocardium. Am J Physiol Heart Circ Physiol. 2008 Jul;295(1):H314-26.
     
    Calpeptin
    Effect of in vivo administration of calpeptin on calpain-, TUNEL-, and gelsolin-associated changes in PO myocardium. Am J Physiol Heart Circ Physiol. 2008 Jul;295(1):H314-26.


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