1. Metabolic Enzyme/Protease Anti-infection
  2. Cathepsin SARS-CoV
  3. Aloxistatin

Aloxistatin  (Synonyms: 阿洛司他丁; E64d; E64c ethyl ester)

目录号: HY-100229 纯度: 99.55%
COA 产品使用指南

Aloxistatin (E64d) 是可渗透细胞,不可逆的广谱半胱氨酸蛋白酶 (cysteine protease) 抑制剂。Aloxistatin (E64d) 可抑制 MERS-CoV。

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Aloxistatin Chemical Structure

Aloxistatin Chemical Structure

CAS No. : 88321-09-9

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10 mM * 1 mL in DMSO ¥1210
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1 mg ¥380
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5 mg ¥1100
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10 mg ¥1900
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25 mg ¥4400
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50 mg ¥7400
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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 50 篇科研文献

WB

    Aloxistatin purchased from MCE. Usage Cited in: Toxicol Appl Pharmacol. 2018 Oct 1;356:159-171.  [Abstract]

    Western blot analysis of PARP and cleaved PARP levels MIA PaCa-2 and PANC-1 cells pre-treated with inhibitors of lysosomal hydrolases (Aloxistatin, 5 μM) for 1 h, followed by a 24-h treatment with Alan (20 μM).
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Aloxistatin (E64d) is a cell-permeable and irreversible broad-spectrum cysteine protease inhibitor. Aloxistatin (E64d) exhibits entry-blocking effect for MERS-CoV.

    IC50 & Target

    Cysteine protease[1]

    体外研究
    (In Vitro)

    Aloxistatin (E64d) 抑制蛋白酶抗性朊病毒蛋白 (PrP-res) 在 ScNB 细胞中的积累,IC50 为 0.5±0.11 μM。对于细胞表面 PrP-sen 检测,PrP-sen 从经过磷脂酰肌醇特异性磷脂酶 C (PIPLC) 处理的培养基中免疫沉淀,以从细胞表面释放脉冲-35S-标记的 PrP-sen[1]
    除了对照细胞,所有细胞的标记培养基中的 Aloxistatin 分别维持在 15 μM。当与 NK-92 或 YT 5 细胞预孵育时,Aloxistatin (E64d) (特异性阻断半胱氨酸蛋白酶,但不阻断丝氨酸蛋白酶,如颗粒酶) 能够完全阻断 CatL 底物 Z-Phe-Arg-aminomethylcoumarin 的周转[2]
    Aloxistatin (E64d) 是一种广谱的细胞渗透性半胱氨酸蛋白酶抑制剂[3]

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

    体内研究
    (In Vivo)

    Aloxistatin (E64d) (灌胃) 会导致豚鼠的脑、CSF 和血浆 Aβ (40) 和 Aβ (42) 剂量依赖性减少。Aloxistatin 还引起脑 CTFβ 的双相剂量依赖性减少。Aloxistatin 导致脑 sAβPPα 剂量依赖性增加。平均 sAβPPα 水平显著高于 5 mg/kg/天或更大的 Aloxistatin 剂量的无剂量组,最高 Aloxistatin 剂量导致 sAβPPα 的最大增加比对照组高约 54%。与 Aβ 效应类似,口服 Aloxistatin 会产生双相剂量依赖性脑组织蛋白酶 B 活性降低。最低有效剂量约为 1 mg/kg/天,最高 Aloxistatin 剂量导致脑组织蛋白酶 B 活性的最大降低,比对照组低约 91%。因此,Aloxistatin 降低豚鼠脑组织蛋白酶 B 活性的方式与化合物抑制组织蛋白酶 B β-分泌酶活性的方式一致[4]
    Aloxistatin (E64d) 抑制大鼠 AT1AR 和 ACE 基因表达的增加。RNH-6270 或 Aloxistatin 的给药减少了 HF 大鼠心肌内冠状动脉超氧化物产生的增加[5]

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

    分子量

    342.43

    Formula

    C17H30N2O5

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    阿洛司他丁

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 125 mg/mL (365.04 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)

    Ethanol 中的溶解度 : ≥ 33.33 mg/mL (97.33 mM)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.9203 mL 14.6015 mL 29.2030 mL
    5 mM 0.5841 mL 2.9203 mL 5.8406 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% EtOH    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (7.30 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 EtOH 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% EtOH    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (7.30 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 EtOH 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: 99.55%

    参考文献
    Cell Assay
    [3]

    Cell proliferation and apoptosis are assessed by staining for a proliferation marker, Ki67, or an apoptotic marker, cleaved caspase 3, following the protocol described above for the polarity markers. MCF10 variants are grown in 3D rBM overlay cultures for 4 days and are treated with 0.1 % DMSO, 5 μM CA074Me or 5 μM Aloxistatin. The percentage of structures that are positive for Ki67 or cleaved caspase 3 is determined by counting a total of 100 structures on two separate coverslips with a Zeiss Axiophot epifluorescent microscope. Structures are considered Ki67 positive if they contained at least one cell staining for Ki67. Structures are considered to be caspase 3 positive if they contained at least one cell that is positive for cleaved caspase 3 and the positive cell(s) is not localized in the center of a developing lumen[3].

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

    Animal Administration
    [4][5]

    Mice and Pigs[4]
    Guinea Pigs (male, Hartley strain, average weight 400 g corresponding to animals about 6 weeks old) are used. Male transgenic mice expressing human AβPP containing the wt β-secretase site and the London mutant β-secretase site sequences are used. Delivering a drug by gavage offers the advantage of accurate dosing but is traumatic and thus only suitable for relatively short dosing periods (up to about a week). Delivery by gavage is used for the guinea pig studies. Aloxistatin is suspended in Me2SO at the indicated concentrations (0.1, 1.0, 5, and 10 mg/kg) and administered by gavage daily using a feeding tube. Vehicle control animals are treated by gavage of Me2SO alone.
    Rats[5]
    Male inbred DS rats are used. Weaned rats are fed laboratory chow containing 0.3% NaCl until 7 weeks of age. DS rats fed an 8% NaCl diet after 7 weeks manifest compensated concentric left ventricular (LV) hypertrophy secondary to hypertension at 12 weeks and a distinct stage of fatal LV failure with lung congestion at 19 weeks. DS rats are therefore fed an 8% NaCl diet from 7 weeks of age and are randomized to an HF group, an Aloxistatin group (10 mg per kg of body mass per day, administered intraperitoneally every other day), or an RNH-6270 group (3 mg/kg per day in chow) from 12 to 19 weeks of age (n=10 for each group). The doses of RNH-6270 (an ARB) and Aloxistatin are determined in preliminary experiments and previous studies. DS rats maintained on the 0.3% NaCl diet served as age-matched controls (control group, n=10). At 19 weeks of age, all of the rats are euthanized by an intraperitoneal overdose of NSC 10816 (50 mg/kg), and the hearts are removed for biological and histological analyses. Arterial blood is collected from the abdominal aorta for the measurement of renin activity. Systolic blood pressure and heart rate are measured in conscious rats from 7 weeks of age, every week, using a noninvasive tail-cuff method. In separate experiments, 12-week-old DS rats, fed a low-salt diet from 7 weeks of age, are given vehicle, RNH-6270, or Aloxistatin in the same manner as in the above experiments (n=5 for each group), and the LV tissues for measuring targeting mRNAs and protein levels are immediately placed in liquid nitrogen and stored at -80°C.

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

    参考文献

    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
    Ethanol / DMSO 1 mM 2.9203 mL 14.6015 mL 29.2030 mL 73.0076 mL
    5 mM 0.5841 mL 2.9203 mL 5.8406 mL 14.6015 mL
    10 mM 0.2920 mL 1.4602 mL 2.9203 mL 7.3008 mL
    15 mM 0.1947 mL 0.9734 mL 1.9469 mL 4.8672 mL
    20 mM 0.1460 mL 0.7301 mL 1.4602 mL 3.6504 mL
    25 mM 0.1168 mL 0.5841 mL 1.1681 mL 2.9203 mL
    30 mM 0.0973 mL 0.4867 mL 0.9734 mL 2.4336 mL
    40 mM 0.0730 mL 0.3650 mL 0.7301 mL 1.8252 mL
    50 mM 0.0584 mL 0.2920 mL 0.5841 mL 1.4602 mL
    60 mM 0.0487 mL 0.2434 mL 0.4867 mL 1.2168 mL
    80 mM 0.0365 mL 0.1825 mL 0.3650 mL 0.9126 mL
    DMSO 100 mM 0.0292 mL 0.1460 mL 0.2920 mL 0.7301 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:
    Aloxistatin
    目录号:
    HY-100229
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