1. Metabolic Enzyme/Protease
  2. Cathepsin
  3. CA-074 methyl ester

CA-074 methyl ester  (Synonyms: CA-074Me)

目录号: HY-100350 纯度: 99.15%
COA 产品使用指南

CA-074 methyl ester 是一种特异性的 Cathepsin B 抑制剂,具有保护神经,抗癌、抗炎等多种生物活性。

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CA-074 methyl ester Chemical Structure

CA-074 methyl ester Chemical Structure

CAS No. : 147859-80-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1049
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1 mg ¥700
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5 mg ¥1200
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10 mg ¥1900
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25 mg ¥3900
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100 mg   询价  

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Top Publications Citing Use of Products

    CA-074 methyl ester purchased from MCE. Usage Cited in: Sci Total Environ. 2023 Apr 13;163460.  [Abstract]

    CA-074 methyl ester (CA; 10 μM; 4 h) significantly reduces the benzo(a)pyrene (BaP) and dibutyl phthalate (DBP) co-exposure-induced expression of p62 and co-localization of p62 and LC3 in macrophages.

    CA-074 methyl ester purchased from MCE. Usage Cited in: Sci Total Environ. 2023 Apr 13;163460.  [Abstract]

    CA-074 methyl ester (CA; 10 μM; 4 h) remarkably mitigates the up-regulation of CTSB induced by benzo(a)pyrene (BaP) and dibutyl phthalate (DBP) co-exposure in macrophages.

    CA-074 methyl ester purchased from MCE. Usage Cited in: Ecotoxicol Environ Saf. 2020 Sep 15;201:110831.  [Abstract]

    Representative images of Western blotting in irradiated GC-1 cells pretreated with MG-132 (10 nM, 12 h) and CA-074me (10 μM, 12 h). The expression of Rpl27a is increased and p53 is decreased in the CA-074-me-treated CIR group.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    CA-074 methyl ester is a specific inhibitor of Cathepsin B, which has potent bioactivities such as neuroprotective, anti-cancer, and anti-inflamatory effects.

    IC50 & Target

    Cathepsin B

     

    体外研究
    (In Vitro)

    CA-074Me (5 μM 和 50 μM) 抑制来自 C57BL/6J 和 NOD/ShiLtJ 小鼠的 BMM 细胞中 RANKL 诱导的破骨细胞生成。CA-074Me 在体外 RANKL 刺激后 24 小时内发挥其抗破骨细胞作用。CA-074Me 不通过 MAPK-ERK 信号级联发挥其抗破骨细胞作用。CA-074Me 抑制 RANKL 刺激后的 c-FOS 上调和随后的 NFATc1 自身扩增[2]
    CA-074Me 减少 CVB1诱导的细胞凋亡[3]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    处理前和处理后,CA074-me (1 μg、10 μg) 可预防全脑 I/R 损伤诱导的海马 CA1 神经元程序性坏死。溶酶体膜的破裂和组织蛋白酶-B 的渗漏,这被 CA074-me 预处理强烈抑制。RIP3的过表达和核转位以及I/R损伤后NAD+水平的降低也受到抑制,同时CA074-me预处理增强了Hsp70的上调[1]
    CA-074Me (30 mg/kg) 在体内能够抑制破骨细胞生成和骨降解[2]
    在 CVB+CA-074Me (4 mg/kg/day im) 豚鼠组中,与 CVB+None 组相比,炎症评分显著降低。与假手术组相比,CVB+CA-074Me组CD8+T细胞数量减少[3]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    分子量

    397.47

    Formula

    C19H31N3O6

    CAS 号
    性状

    固体

    颜色

    White to off-white

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 100 mg/mL (251.59 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.5159 mL 12.5796 mL 25.1591 mL
    5 mM 0.5032 mL 2.5159 mL 5.0318 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.29 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.29 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.15%

    参考文献
    Kinase Assay
    [2]

    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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    RANKL (0.08 mg/kg) with and without CA-074Me (10 mg/kg or 30 mg/kg) are mixed in sterile, nonimmunogenic 1% Extracel-HP gel. The gel is composed of thiol-modified sodium hyaluronate, thiol-modified heparin, thiol-modified gelatin, and degassed deionized sterile water. The hydrogel mixture is prepared in an aseptic hood using a sterile syringe. The control sham hydrogel contained sterile Phosphate Buffered Saline (PBS) without any cytokines. The osteolysis group is given 0.08 mg/kg RANKL in a hydrogel to induce pathologic bone loss. The hydrogel-only, hydrogel-RANKL, and hydrogel-RANKL-CA-074Me mixture is injected into 8-week old male mice calvarium in an aseptic hood (n = 5) following general anesthesia (80 mg/kg of ketamine and 7 mg/kg of xylazine). After four days, the calvaria are excised, fixed in 4% formaldehyde for 24 h, decalcified in 20% EDTA for one week, and sectioned into slides from paraffin blocks. The slides undergo Tartrate-Resistant Acid Phosphatase (TRAP) staining to identify osteoclasts.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献

    CA-074 methyl ester 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 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 1.2580 mL 2.5159 mL 6.2898 mL
    15 mM 0.1677 mL 0.8386 mL 1.6773 mL 4.1932 mL
    20 mM 0.1258 mL 0.6290 mL 1.2580 mL 3.1449 mL
    25 mM 0.1006 mL 0.5032 mL 1.0064 mL 2.5159 mL
    30 mM 0.0839 mL 0.4193 mL 0.8386 mL 2.0966 mL
    40 mM 0.0629 mL 0.3145 mL 0.6290 mL 1.5724 mL
    50 mM 0.0503 mL 0.2516 mL 0.5032 mL 1.2580 mL
    60 mM 0.0419 mL 0.2097 mL 0.4193 mL 1.0483 mL
    80 mM 0.0314 mL 0.1572 mL 0.3145 mL 0.7862 mL
    100 mM 0.0252 mL 0.1258 mL 0.2516 mL 0.6290 mL
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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    产品名称:
    CA-074 methyl ester
    目录号:
    HY-100350
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