1. NF-κB
  2. IKK
  3. Amlexanox

Amlexanox  (Synonyms: 氨来呫诺; AA673; Amoxanox; CHX3673)

目录号: HY-B0713 纯度: 99.88%
COA 产品使用指南

Amlexanox (AA673; Amoxanox; CHX3673) 是特异性的 IKKεTBK1 抑制剂,IC50 值为 1-2 μM。

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Amlexanox Chemical Structure

Amlexanox Chemical Structure

CAS No. : 68302-57-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥614
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1 mg ¥174
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5 mg ¥348
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10 mg ¥558
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50 mg ¥800
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100 mg ¥1000
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Top Publications Citing Use of Products

    Amlexanox purchased from MCE. Usage Cited in: Exp Lung Res. 2023 Jan 31;1-14.  [Abstract]

    Amlexanox (25 μM; pretreat for 2 h) reverses HDM-induced MUC5AC overexpression in human bronchial epithelial cells.

    Amlexanox purchased from MCE. Usage Cited in: PLoS Pathog. 2018 Mar 8;14(3):e1006948.   [Abstract]

    HeLa cells are treated with AS (0.5 mM) for 30 min and subsequently treated with or without CHX in the presence of AS for another 1 h.

    Amlexanox purchased from MCE. Usage Cited in: PLoS Pathog. 2018 Mar 8;14(3):e1006948.   [Abstract]

    Cell lysates are analyzed via western blot using anti-HN and anti-GAPDH antibodies in CHX trestment.

    Amlexanox purchased from MCE. Usage Cited in: PLoS Pathog. 2018 Mar 8;14(3):e1006948.   [Abstract]

    HeLa cells are treated with AS (0.5 mM) for 30 min and subsequently treated with or without CHX in the presence of AS for another 1 h.

    Amlexanox purchased from MCE. Usage Cited in: Cell Death Dis. 2017 Aug 31;8(8):e3022.  [Abstract]

    Amlexanox reduces the protein expression of the Hippo pathway through downregulation of IKBKE. (a) U87 and U251 cells are treated with various concentrations of Amlexanox for 72 h. The cells are harvested, and the effects of Amlexanox on the protein expression of the Hippo pathway are detected by western blot. (b) U87 and U251 cells are treated with Amlexanox at 150 μM for 24, 48 and 72 h. Cell lysates are collected, and the protein expression are detected by western blot.

    查看 IKK 亚型特异性产品:

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Amlexanox (AA673; Amoxanox; CHX3673) is a specific inhibitor of IKKε and TBK1, and inhibits the IKKε and TBK1 activity determined by MBP phosphorylation with an IC50 of approximately 1-2 μM.

    IC50 & Target[1]

    IKKε

    1-2 μM (IC50)

    TBK1

    1-2 μM (IC50)

    体外研究
    (In Vitro)

    Amlexanox 增加 3T3-L1 脂肪细胞中 Ser172 上 TBK1 的磷酸化,并阻断聚肌胞苷:聚胞苷酸 (poly I:C) 刺激的干扰素反应因子 3 (IRF3) 的磷酸化,IRF3 是 IKKεTBK1 的假定底物[1]
    Amlexanox 在体外环境中有效抑制肥大细胞、嗜碱性粒细胞和嗜中性粒细胞释放组胺和白三烯,这可能是通过增加炎症细胞中的细胞内环 AMP 含量、膜稳定作用或抑制钙流入[2]
    在原代骨髓来源的巨噬细胞 (BMM) 中,amlexanox 抑制破骨细胞形成和骨吸收。在分子水平上,amlexanox 抑制 RANKL 诱导的核因子-κB (NF-κB)、丝裂原活化蛋白激酶 (MAPK)、c-Fos 和 NFATc1 的激活。Amlexanox 降低破骨细胞特异性基因的表达,包括 TRAP、MMP9、组织蛋白酶 K 和 NFATc1[3]

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

    体内研究
    (In Vivo)

    Amlexanox (100 mg/kg,po) 预防和逆转饮食诱导或遗传性肥胖,并在肥胖小鼠中产生可逆的体重减轻。Amlexanox 还导致这些小鼠的脂肪组织质量显著减少,循环脂联素增加。Amlexanox (25 mg/kg) 可显著改善已建立 DIO 的小鼠的胰岛素敏感性,经过 4 周的处理后,amlexanox 可显著改善葡萄糖[1]
    Amlexanox 在第一次使用糊剂之前和每次都被证明可以抑制即时和之后的评估。分类量表也是迟发型超敏反应[2]
    Amlexanox (20 mg/kg) 增强 BMSCs 的成骨细胞分化。在卵巢切除 (OVX) 小鼠模型中,amlexanox 通过抑制破骨细胞活性来防止 OVX 诱导的骨质流失[3]

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

    Clinical Trial
    分子量

    298.29

    Formula

    C16H14N2O4

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    氨来呫诺;氨来占司;安来诺克司;氨来占诺

    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 1 year
    -20°C 6 months
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 100 mg/mL (335.24 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 3.3524 mL 16.7622 mL 33.5244 mL
    5 mM 0.6705 mL 3.3524 mL 6.7049 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, 1 years; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

    • 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 (8.38 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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (8.38 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,此方案实验周期在半个月以上的动物实验酌情使用。

      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玉米油中,混合均匀。

    以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 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: 0.5% CMC-Na/saline water

      Solubility: 20 mg/mL (67.05 mM); 悬浊液; 超声助溶

    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: 99.88%

    参考文献
    Kinase Assay
    [1]

    The in vitro kinase assays is performed by incubating purified kinase (IKKε or TBK1) in kinase buffer containing 25 mM Tris (pH7.5), 10 mM MgCl2, 1 mM DTT, and 10 µM ATP for 30 minutes at 30°C in the presence of 0.5 µCi γ-[32P]-ATP and 1 µg MBP per sample as a substrate. The kinase reaction is stopped by adding 4x sodium dodecyl sulfate (SDS) sample buffer and boiling for 5 minutes at 95°C. Supernatants are resolved by SDS-polyacrylamide gel electrophoresis, transferred to nitrocellulose, and analyzed by autoradiography using a Typhoon 9410 phosphorimager.

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

    Cell Assay
    [3]

    To examine cell proliferation, a Cell Counting Kit-8 is used according to the manufacturer’s instructions. BMMs are seeded at a density of 5×103 cells/well in 96-well plates. After 24 hours, cells are treated with different concentrations of AmLexanox (0, 1.5, 3, 6, 12, 25 μM) every 2 days in the presence of M-CSF (30 ng/mL) for 7 days. After 1, 3, 5 and 7 days, the culture medium is replaced by the medium containing 10% CCK-8 and cells are incubated at 37°C for an additional 2 h. The absorbance is then measured at a wavelength of 450 nm on an ELX800 absorbance microplate reader.

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

    Animal Administration
    [1]

    Wildtype male C57BL/6 mice are fed with a HFD consisting of 45% of calories from fat starting at eight weeks of age for 12-24 weeks, while ND C57BL/6 controls are maintained on normal chow diet consisting of 4.5% fat. C57BL/6 diets are fed containing ω-3 fatty acids. Rosiglitazone treatment is administered for three weeks by addition of the compound to the diet in mice that have been on HFD for 16 weeks. Each mouse consumes on average 3.5 mg per kg rosiglitazone per day. AmLexanox is administered by daily oral gavage. For the prevention groups, amLexanox (25 mg per kg or 100 mg per kg) administration is begun concurrently with HFD feeding at eight weeks of age. For the treatment groups, 25 mg per kg amLexanox treatment is begun at 20 weeks of age after 12 weeks of HFD. To test the effect of amLexanox withdrawal, mice in the treatment group are switched from amLexanox gavage to vehicle control after eight weeks of amLexanox treatment. Control and ob/ob mice are fed with a normal chow diet and gavaged with 100 mg per kg amLexanox or vehicle control beginning at ten weeks of age. Animals are housed in a specific pathogen-free facility with a 12-hour light/12-hour dark cycle and given free access to food and water.

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

    参考文献

    Amlexanox 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, 1 years; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.3524 mL 16.7622 mL 33.5244 mL 83.8111 mL
    5 mM 0.6705 mL 3.3524 mL 6.7049 mL 16.7622 mL
    10 mM 0.3352 mL 1.6762 mL 3.3524 mL 8.3811 mL
    15 mM 0.2235 mL 1.1175 mL 2.2350 mL 5.5874 mL
    20 mM 0.1676 mL 0.8381 mL 1.6762 mL 4.1906 mL
    25 mM 0.1341 mL 0.6705 mL 1.3410 mL 3.3524 mL
    30 mM 0.1117 mL 0.5587 mL 1.1175 mL 2.7937 mL
    40 mM 0.0838 mL 0.4191 mL 0.8381 mL 2.0953 mL
    50 mM 0.0670 mL 0.3352 mL 0.6705 mL 1.6762 mL
    60 mM 0.0559 mL 0.2794 mL 0.5587 mL 1.3969 mL
    80 mM 0.0419 mL 0.2095 mL 0.4191 mL 1.0476 mL
    100 mM 0.0335 mL 0.1676 mL 0.3352 mL 0.8381 mL
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    • Do most proteins show cross-species activity?

      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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    目录号:
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