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

Apocynin  (Synonyms: Acetovanillone)

Cat. No.: HY-N0088 Purity: 99.96%
COA Handling Instructions

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

For research use only. We do not sell to patients.

Apocynin Chemical Structure

Apocynin Chemical Structure

CAS No. : 498-02-2

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Solid + Solvent
10 mM * 1 mL in DMSO
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Customer Review

Based on 17 publication(s) in Google Scholar

Other Forms of Apocynin:

Top Publications Citing Use of Products

    Apocynin purchased from MedChemExpress. 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 MedChemExpress. 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.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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].

    In Vitro

    Apocynin (100 μM; 1-7, 14 days) shows a significant increase in the expression level of an osteogenic marker in the aging BMSCs after osteogenic induction[3].
    Apocynin (1, 10, 100 μM, 0-48h ) has selective inhibition the proliferation and adhesion to fibronectin of v-H-ras-transformed 3Y1 cells[4].
    Apocynin (1, 10, 100 μM; 3, 6, 12 h) decreases the intracellular reactive oxygen species (ROS) level in HR-3Y1-2 but not 3Y1 cells. [4].

    MedChemExpress (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.
    In Vivo

    Apocynin (0.1 mg/kg/day, i.p., three times per week for 3 months) increases bone mineral density and total bone volume in SAMP6 mice[3].
    Apocynin (5 mg/kg, i.p.) reduces the degree of lung injury and attenuates the degree of acute inflammation in the Carrageenan (HY-125474)-induced pleurisy mice[5].

    MedChemExpress (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
    Molecular Weight

    166.17

    Formula

    C9H10O3

    CAS No.
    Appearance

    Solid

    Color

    Off-white to gray

    SMILES

    CC(C1=CC=C(O)C(OC)=C1)=O

    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (601.79 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 3.33 mg/mL (20.04 mM; ultrasonic and warming and heat to 60°C)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    Volume (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (15.04 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (15.04 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.96%

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 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

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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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