產(chǎn)品屬性:
產(chǎn)品名稱(chēng) | 規(guī)格 | CAS號(hào) | 型號(hào) |
Calpain Inhibitor XII | 1mg 5mg 10mg | 181769-57-3 | EY-Y0163985 |
Cas No.181769-57-3
別名 Z-L-Nva-CONH-CH2-2-Py
化學(xué)名 [3-methyl-1-[[[1-[oxo[(2-pyridinylmethyl)amino]acetyl]butyl]amino]carbonyl]butyl]-carbamic acid, phenylmethyl ester
分子式 C26H34N4O5
分子量 482.6
溶解度 ≤16mg/ml in ethanol;16mg/ml in DMSO;20mg/ml in dimethyl formamide
儲(chǔ)存條件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產(chǎn)品描述:
Ki: 19 nM for μ-calpain
Calpain Inhibitor XII is a reversible and selective inhibitor of calpain I.
Calpain is a protein belonging to the family of calcium-dependent, non-lysosomal cysteine proteases expressed ubiquitously in mammals and many other organisms. Calpain inhibitors have been used to study the role of calpains in diverse processes, including neutrophil chemotaxis, neuronal signaling, and cardiac response to injury.
In vitro: A series of new dipeptidyl alpha-keto amides of the general structure R1-L-Leu-D,L-AA-CONH-R2 including Calpain Inhibitor XII were synthesized and evaluated as inhibitors for the cysteine proteases calpain I, calpain II, and cathepsin B. Calpain II was more sensitive to these inhibitors Calpain Inhibitor XII than calpain I. Calpain I was also effectively inhibited by Calpain Inhibitor XII, but lower Ki values than with calpain II. Cathepsin B was weakly inhibited by Calpain Inhibitor XII. The best calpain I inhibitor in this study was Calpain Inhibitor XII with Ki value of 19 nM [1].
In vivo: Up to now, there is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Li, Z. ,Ortega-Vilain, A.C.,Patil, G.S., et al. Novel peptidyl α-keto amide inhibitors of calpains and other cysteine proteases. Journal of Medicinal Chemistry 39(20), 4089-4098 (1996).
關(guān)鍵字: 181769-57-3;C26H34N4O5;Calpain Inhibitor XI;
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