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E 64c {[allProObj[0].p_purity_real_show]}

货号:A602643 同义名: Loxistatin acid;NSC 694279

Loxistatin acid, a derivative of E-64, is an irreversible and membrane-permeant cysteine protease inhibitor.

E 64c 化学结构 CAS号:76684-89-4
E 64c 化学结构
CAS号:76684-89-4
E 64c 3D分子结构
CAS号:76684-89-4
E 64c 化学结构 CAS号:76684-89-4
E 64c 3D分子结构 CAS号:76684-89-4
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E 64c 纯度/质量文件 产品仅供科研

货号:A602643 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Cysteine Protease 其他靶点 纯度
Z-FA-FMK 99%+
Leupeptin hemisulfate 97%
PMSF 95%
PD 151746 +

μ-Calpain, IC50: 260 nM

m-calpain, IC50: 5.33 μM

98%
Odanacatib ++++

Cathepsin K (human), IC50: 0.2 nM

Cathepsin K (rabbit), IC50: 1 nM

99%+
E-64 +++

Cysteine protease, IC50: 9 nM

99%+
E 64c 95%
E-64d 99%+
MG-101 98%+
Calpeptin ++

Calpain I (porcine erythrocytes), ID50: 52 nM

Calpain II (porcine kidney), ID50: 40 nM

98%+
Cathepsin inhibitor 1 +++

Cathepsin L2, pIC50: 5.5

Cathepsin L, pIC50: 7.9

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

E 64c 生物活性

靶点
  • Cysteine Protease

描述 E-64c is a derivative of a naturally occurring epoxide that inhibits cysteine proteases, particularly effective against papain. This inhibition is characterized by the hydrogen bonding and hydrophobic interactions between the ligands and the conserved residues within the catalytic binding site[1]. E-64c has been identified as a primary structure for the creation of irreversible inhibitors targeting cathepsin C[2].

E 64c 动物研究

Animal study The half-life (t-1/2) of E-64c in plasma is 0.48 hours. At this dosage, E-64c does not exhibit hemodynamic effects. Statistical analysis using two-way ANOVA reveals that both reperfusion and E-64c independently have significant effects on infarct size. The reduction in creatine phosphokinase (CPK) is marginally lower in the E-64c treated groups compared to the vehicle-injected groups. The limited efficacy of E-64c might be due to its early administration and the relatively short half-life. Given the established effectiveness of NCO-700, the results suggest that E-64c may have a modest yet positive impact on reducing infarct size and CPK levels[3].

E 64c 参考文献

[1]Khan MS, et al. Design, synthesis, evaluation and thermodynamics of 1-substituted pyridylimidazo[1,5-a]pyridine derivatives as cysteine protease inhibitors. PLoS One. 2013 Aug 5;8(8):e69982.

[2]Radzey H, et al. E-64c-hydrazide: a lead structure for the development of irreversible cathepsin C inhibitors. ChemMedChem. 2013 Aug;8(8):1314-21.

[3]Toda G, et al. Calcium-activated neutral protease inhibitor (E-64c) and reperfusion for experimental myocardial infarction. Jpn Heart J. 1989 May;30(3):375-86.

E 64c 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.18mL

0.64mL

0.32mL

15.90mL

3.18mL

1.59mL

31.81mL

6.36mL

3.18mL

E 64c 技术信息

CAS号76684-89-4
分子式C15H26N2O5
分子量 314.377
别名 Loxistatin acid;NSC 694279;EP 475
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Store in freezer, under -20°C

溶解度

DMSO: 250 mg/mL(795.22 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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