| CalpeptinCa2+-dependent protease,calpain inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 98.00%
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Chemical structure
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| Cas No. | 117591-20-5 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | benzyl N-[4-methyl-1-oxo-1-(1-oxohexan-2-ylamino)pentan-2-yl]carbamate | ||
| Canonical SMILES | CCCCC(C=O)NC(=O)C(CC(C)C)NC(=O)OCC1=CC=CC=C1 | ||
| Formula | C20H30N2O4 | M.Wt | 362.47 |
| Solubility | ≥36.2mg/mL in EtOH | Storage | Desiccate at 4°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
IC50: 5 nM for human calpain 1
Calpeptin is a calpain inhibitor.
As a calcium-dependent intracellular cysteine protease, calpain plays an key role in various cellular processes including cell differentiation, growth and apoptosis. In rheumatoid arthritis patients, over-expression of calpains are observed in arthritic synovial fluid and are thought to play critical roles in various cellular processes.
In vitro: 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 [1].
In vivo: The preventive effect of calpeptin has been examined on bleomycin-induced pulmonary fibrosis in mice. Histological examinations and quantitative measurements of related proteins in bleomycin-treated mouse lung tissues with or without calpeptin were performed. Calpeptin histologically ameliorated bleomycininduced pulmonary fibrosis in mice. Results showed that calpeptin decreased the expression of IL-6, TGF-b1, angiopoietin-1 and collagen type Ia1 mRNA in mouse lung tissues [1].
Clinical trial: N/A
Reference:[1] Tabata C,Tabata R,Nakano T. The calpain inhibitor calpeptin prevents bleomycin-induced pulmonary fibrosis in mice. Clin Exp Immunol.2010 Dec;162(3):560-7.
