1. Metabolic Enzyme/Protease
  2. NADPH Oxidase
  3. Apocynin

Apocynin  (Synonyms: 香草乙酮; Acetovanillone)

目录号: HY-N0088 纯度: 99.96%
COA 产品使用指南

Apocynin 是选择性的 NADPH-氧化酶 抑制剂,IC50 为 10 μM。Apocynin 改善 Carrageenan (HY-125474) 诱导的小鼠胸膜炎模型中的急性肺部炎症。Apocynin 也可用于癌症研究。Apocynin 逆转间充质干细胞的衰老过程,促进成骨,增加骨量。

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Apocynin Chemical Structure

Apocynin Chemical Structure

CAS No. : 498-02-2

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10 mM * 1 mL in DMSO ¥500
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5 g ¥800
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Top Publications Citing Use of Products

    Apocynin purchased from MCE. Usage Cited in: Free Radic Biol Med. 2021 Mar 16;S0891-5849(21)00113-1.  [Abstract]

    Western Blots show that ZO-1 is significantly recovered with pretreatment of Apocynin and pathway inhibitors compared with CCL8 treatment alone. The result shows that with pretreatment of Apocynin, the increased phosphorylation p65 level induced by CCL8 is significantly weakened.

    Apocynin purchased from MCE. Usage Cited in: Redox Biol. 2018 May;15:418-434.  [Abstract]

    DPH oxidase inhibitor attenuates TSH-induced oxidative stress in HUVECs. NADPH oxidase inhibitor (Apocynin, 100 μM) is used to confirm the effects of NADPH oxidase activation in TSH-induced intracellular oxidative stress.
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Apocynin is a selective NADPH-oxidase inhibitor with an IC50 of 10 μM[1][2]. Apocynin improves acute lung inflammation in Carrageenan (HY-125474)-induced pleurisy mice model[3]. Apocynin can also be used for cancer research[4]. Apocynin reverses the aging process in mesenchymal stem cells to promote osteogenesis and increases bone mass[5].

    体外研究
    (In Vitro)

    Apocynin (100 μM,1-7,14 天) 在诱导成骨后,使老化 BMSC 细胞中的成骨标记物表达水平显著增加[3]
    Apocynin (1,10,100 μM;48 小时) 选择性抑制 v-H-ras 转染的 3Y1 细胞的增殖和对纤维连接蛋白的粘附[4]
    Apocynin (1,10,100 μM;3,6,12 小时) 降低 HR-3Y1-2 细胞而非 3Y1 细胞的细胞内活性氧(ROS)水平[4]

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

    Western Blot Analysis[3]

    Cell Line: Bone marrow stromal cells (BMSCs)
    Concentration: 100 μM
    Incubation Time: 1-7,14 days
    Result: Increased the expression levels of the “stemness markers” Nanog and Oct-4.
    Decreased the expression levels of p53, p21 and p16 at both the mRNA level and protein level.
    Increased the expression of sox-2 and klf-4 by 82.4% and 38.7%, respectively, compared with the negative control group.
    Reduced the expression of NADPH oxidase by 66.5% compared with the negative control.
    Had no change in the cell cycle or proliferation.
    Ddecreased the percentage of SA-β –gal-positive (green-stained) cells was by 42.5%.
    Increased the expression levels of four pivotal osteogenic markers (Runx2, OSX, Ocn, and Col1).

    Cell Proliferation Assay[4]

    Cell Line: HR-3Y1-2, 3Y1 cells
    Concentration: 0, 1, 10, or 100 μM
    Incubation Time: 48h
    Result: Inhibited the proliferation of HR-3Y1-2 but not 3Y1 cells at 10μM and 100μM.

    RT-PCR[3]

    Cell Line: HR-3Y1-2, 3Y1 cells
    Concentration: 0, 1, 10, or 100 μM
    Incubation Time: 24, 36, 48 h
    Result: Selectively down-regulated 1-integrin cell surface expression on the HR-3Y1-2 cells.
    Decreased adhesion of HR-3Y1-2 cells to fibronectin-coated plates.
    体内研究
    (In Vivo)

    Apocynin (0.1 mg/kg/天,腹腔注射,每周 3 次,持续 3 个月) 在 SAMP6小鼠中增加骨矿物质密度和总骨量[3]
    Apocynin (5 mg/kg,腹腔注射) 可降低 Carrageenan (HY-125474) 诱导的胸膜炎小鼠的肺损伤程度,减轻急性炎症程度[5]

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

    Animal Model: SAMP6 mouse model (Pharmacokinetic assay)[3]
    Dosage: 0.1 mg/kg/day
    Administration: Intraperitoneal injection (i.p.), three times per week, for 3 months
    Result: Showed a higher bone value and exhibited a lower percentage of SA-β -gal positive cells than the control group.
    Increased the expression of Ki67 and Oct-4 mRNA.
    Altered the osteoblast-osteoclast balance in bone and promoted the activity of osteoblasts.
    Animal Model: Carrageenan (HY-125474)-induced pleurisy in male adult CD1 mice [5]
    Dosage: 5 mg/kg
    Administration: Intraperitoneal injection (i.p.)
    Result: Blocked NADPH oxidase activation and attenuated neutrophil infiltration and lipid peroxidation in the lung tissue.
    Reduced the degree of PARP activation and the degree of IL-1b expression.
    Prevented carrageenan-induced IkB-a degradation and reduced the levels of NF-kB p65.
    Attenuated this iNOS expression,reduced the degree of positive staining for Fas ligand in the lung tissues.
    Inhibited cells apoptosis in carrageenan-treated mice.
    Prevented Bax expression and reduced the degree of positive staining for Bax.
    Attenuated carrageenan-induced inhibition of Bcl-2 expression and the loss of positive staining for Bcl-2 in mice subjected to carrageenan-induced pleurisy.
    Reduced the level of pERK1/2 and p38 expression.
    Clinical Trial
    分子量

    166.17

    Formula

    C9H10O3

    CAS 号
    性状

    固体

    颜色

    Off-white to gray

    中文名称

    罗布麻宁;加拿大麻素;夹竹桃麻素;香草乙酮;乙酰酮

    结构分类
    初始来源
    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 : ≥ 100 mg/mL (601.79 mM; 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 : 3.33 mg/mL (20.04 mM; 超声助溶 (<60°C))

    * "≥" 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 6.0179 mL 30.0897 mL 60.1793 mL
    5 mM 1.2036 mL 6.0179 mL 12.0359 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。

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    • 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 (15.04 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 (15.04 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: 99.96%

    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
    H2O / DMSO 1 mM 6.0179 mL 30.0897 mL 60.1793 mL 150.4483 mL
    5 mM 1.2036 mL 6.0179 mL 12.0359 mL 30.0897 mL
    10 mM 0.6018 mL 3.0090 mL 6.0179 mL 15.0448 mL
    15 mM 0.4012 mL 2.0060 mL 4.0120 mL 10.0299 mL
    20 mM 0.3009 mL 1.5045 mL 3.0090 mL 7.5224 mL
    DMSO 25 mM 0.2407 mL 1.2036 mL 2.4072 mL 6.0179 mL
    30 mM 0.2006 mL 1.0030 mL 2.0060 mL 5.0149 mL
    40 mM 0.1504 mL 0.7522 mL 1.5045 mL 3.7612 mL
    50 mM 0.1204 mL 0.6018 mL 1.2036 mL 3.0090 mL
    60 mM 0.1003 mL 0.5015 mL 1.0030 mL 2.5075 mL
    80 mM 0.0752 mL 0.3761 mL 0.7522 mL 1.8806 mL
    100 mM 0.0602 mL 0.3009 mL 0.6018 mL 1.5045 mL

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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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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