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CA-074 methyl ester

产品编号 T3420 CAS 147859-80-1

别名: Cathepsin B Inhibitor IV, CA-074Me

CA-074 methyl ester (Cathepsin B Inhibitor IV) 是Cathepsin B 的选择性抑制剂，具有保护神经、抗炎、抗癌等多种作用。

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CA-074 methyl ester, CAS 147859-80-1

规格	价格/CNY	货期
1 mg	￥ 413	现货
2 mg	￥ 588	现货
5 mg	￥ 980	现货
10 mg	￥ 1,590	现货
25 mg	￥ 3,230	现货
50 mg	￥ 4,630	现货
100 mg	￥ 6,490	现货
1 mL * 10 mM (in DMSO)	￥ 867	现货

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选择批次

纯度: 99.58%

纯度: 99.49%

纯度: 97.26%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	CA-074 methyl ester (Cathepsin B Inhibitor IV) is a specific inhibitor of Cathepsin B with neuroprotective, anti-cancer, and anti-inflammatory effects.
体外活性	CA-074Me is able to inhibit cathepsin L within living HL-60 cells and bloodstream forms of Trypanosoma brucei brucei, but does not inhibit cathepsin L in the absence of thiols. CA-074Me is converted into CA-074 by intracellular esterasesand is, therefore, able to inhibit cathepsin B in GSH-depleted HL-60 cell. It is suggested that CA-074 rather than CA-074Me should be used to selectively inhibit cathespsin B within living cells[1]. Myotube size and number and induced levels of fusion-related creatine phosphokinase activity and myosin heavy-chain protein are reduced from 30 to 50% in CA074Me-treated myoblasts. These reductions are also dose related. Micromolar concentrations of CA074Me inhibit catB activity in differentiating myoblasts[2].
体内活性	Administration of CA074Me to the London APP mice results in significant improvement in memory deficit, reduces amyloid plaque load in brain, reduces levels of Aβ40 and Aβ42 in brain, and reduces C-terminal β-secretase fragment (CTFβ) derived from APP by β-secretase when compared with untreated control animals. It has no effect on any of these parameters in mice expressing the Swe mutant β-secretase site of APP (in Swedish/London APP mice). In vivo icv administration of CA074Me to normal guinea pigs results in substantial reduction of brain Aβ levels and inhibits β-secretase activity[3].
激酶实验	After seven days of cell culture and osteoclast generation, the media is removed and washed three times with PBS. BMMs are fixed with a fixing solution supplied by the manufacturer. The cells are incubated at 37°C with a solution containing deionized water, Fast Garnet GBC, Napthol phosphate, Acetate, and Tartrate for 1 h. The staining solution is removed, washed with PBS (3×), and air-dried. TRAP positive cells with three or more nuclei across whole culture area are counted as multinucleated osteoclasts using light microscopy.
细胞实验	HL-60 cells are pre-treated for 24 h with 200 μM BSO followed by 60 min with 1 mM DEM. Thereafter, the cells(1×106/ml) are incubated with 100 μM CA-074 or CA-074Me, in the presence of 1% DMSO, 200 μM BSO and 1 mM DEM at 37°C. Control cultures are treated with 1% DMSO alone or with 100 μM Z-FA-DMK in the presence of 200 μM BSO and 1 mM DEM. Untreated HL-60 cells are incubated with 100 μM CA-074 or CA-074Me, in the presence of 1% DMSO at 37°C. Untreated control cultures are incubated with 1% DMSO alone or with 100 μM Z-FA-DMK. After 2 h incubation, cells are washed three times with PBS/1% glucose and lysed in 100 mM citrate, pH 5.0, 2% Chaps (106 cells/100 μl). Subsequently, the lysate is centrifuged and the clarified supernatant used to assay for proteolytic activity.(Only for Reference)

别名	Cathepsin B Inhibitor IV, CA-074Me
分子量	397.47
分子式	C19H31N3O6
CAS No.	147859-80-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 73 mg/mL (183.6 mM)

H2O: 72 mg/mL (181.1 mM)

Ethanol: 73 mg/mL (183.6 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO / H2O / Ethanol	1 mM	2.5159 mL	12.5796 mL	25.1591 mL	62.8978 mL
	5 mM	0.5032 mL	2.5159 mL	5.0318 mL	12.5796 mL
	10 mM	0.2516 mL	1.258 mL	2.5159 mL	6.2898 mL
	20 mM	0.1258 mL	0.629 mL	1.258 mL	3.1449 mL
	50 mM	0.0503 mL	0.2516 mL	0.5032 mL	1.258 mL
	100 mM	0.0252 mL	0.1258 mL	0.2516 mL	0.629 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Dietmar Steverding, et al. The Open Enzyme Inhibition Journal. 2011, 4:11-16. 2. Jane DT, et al. Biochem Cell Biol. 2002, 80(4):457-65.

文献引用

1. Wang Y, Chen Y Y, Gao G B, et al.Polyphyllin D “Punctures” Hypertrophic Lysosomes to Reverse Drug Resistance of Hepatocellular Carcinoma by Targeting Acid Sphingomyelinase.Molecular Therapy.2023

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

CA-074 methyl ester 147859-80-1 Proteases/Proteasome Cysteine Protease CA074 methyl ester Inhibitor Cathepsin Cathepsin B Inhibitor IV inhibit CA 074 methyl ester CA-074Me inhibitor

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CA-074 methyl ester

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords