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Calpain Inhibitor XII
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Calpain Inhibitor XII图片
CAS NO:181769-57-3
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Calpain Inhibitor XII 是一种可逆的选择性 calpain I 抑制剂 (μ-calpain, Ki=19 nM)。
Cas No.181769-57-3
别名Z-L-Nva-CONH-CH2-2-Py
化学名[3-methyl-1-[[[1-[oxo[(2-pyridinylmethyl)amino]acetyl]butyl]amino]carbonyl]butyl]-carbamic acid, phenylmethyl ester
Canonical SMILESO=C(NC(CC(C)C)C(NC(CCC)C(C(NCC1=NC=CC=C1)=O)=O)=O)OCC2=CC=CC=C2
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
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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).

 
 
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