1. Metabolic Enzyme/Protease
  2. NADPH Oxidase
  3. ML171

ML171  (Synonyms: 2-Acetylphenothiazine; 2-APT)

Cat. No.: HY-12805 Purity: 99.82%
COA Handling Instructions

ML171 (2-Acetylphenothiazine;2-APT) is a potent and selective NADPH oxidase 1 (Nox1) inhibitor that blocks Nox1-dependent ROS generation, with an IC50 of 0.25 μM in HEK293-Nox1 confirmatory assay.

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

ML171 Chemical Structure

ML171 Chemical Structure

CAS No. : 6631-94-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 33 In-stock
Solution
10 mM * 1 mL in DMSO USD 33 In-stock
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100 mg USD 30 In-stock
500 mg USD 60 In-stock
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Customer Review

Based on 16 publication(s) in Google Scholar

Top Publications Citing Use of Products

    ML171 purchased from MedChemExpress. Usage Cited in: Inflammation. 2023 Feb 20.  [Abstract]

    In rat NP cells, ML171 inhibits the expression of catabolic markers MMP13, ADAMTS4, ADAMTS5, and pyroptotic markers NLRP3, GSDMD-NT, and cleaved-caspase-1, as well as incresaes the expression of ECM anabolic markers COL2A and ACAN, by inhibiting overexpression of BRD9 (Fig. c and d).
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    ML171 (2-Acetylphenothiazine;2-APT) is a potent and selective NADPH oxidase 1 (Nox1) inhibitor that blocks Nox1-dependent ROS generation, with an IC50 of 0.25 μM in HEK293-Nox1 confirmatory assay.

    IC50 & Target

    NOX1

     

    In Vitro

    Nox1-dependent ROS generation has been shown to play a pivotal role in cell signaling, cell growth, angiogenesis, motility and blood pressure regulation. ML171 strongly blocks ROS generation in HT29 cells (IC50=0.129 μM) and only increasing over-expression of Nox1 can overcome the blockage of ROS generation caused by ML171 treatment in HEK293 cell system reconstituted with all the components required Nox1-dependent ROS generation. ML171 efficiently blocks ROS production measured by carboxy-H2-DCFDA staining as well as DPI used as a positive control. When ML171 is tested in HEK293-Nox1 reconstituted cell system, higher potency in blocking Nox1-dependent ROS generation is observed compared with the parental compound[1].

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

    Molecular Weight

    241.31

    Formula

    C14H11NOS

    CAS No.
    Unlabeled CAS

    Appearance

    Solid

    Color

    Yellow to orange

    SMILES

    CC(C1=CC=C2SC3=CC=CC=C3NC2=C1)=O

    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 : ≥ 64 mg/mL (265.22 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 4.1440 mL 20.7202 mL 41.4405 mL
    5 mM 0.8288 mL 4.1440 mL 8.2881 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.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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 (10.36 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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (10.36 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    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: 99.82%

    References
    Cell Assay
    [1]

    HT29 cells are cultured in 150 mm diameter plate and when 70-80% confluence is reached, cells are trypsinized, harvested in HBSS and counted. 4×104 cells are dispensed into individual wells in 30 μL final volume (384 well plates) by using a robotic liquid handler. Cells are treated for 60 min at 37°C with 50 nL of DPI, DMSO and library compounds (including ML171) which are automatically dispensed into individual wells from their respective assay plates. This will correspond to a final concentration of 10 μM DPI or library compounds (ML171), and 0.1% DMSO. 20 μL of a mixture containing 200 μM luminol plus 0.32 units of HRP (final concentration) is added. Luminescence is quantified using a 384-well plate luminometer. The data output consisting of the emission intensities for each well is imported into a spread-sheet program (such as Excel) for further processing. As designed, compounds that inhibit Nox1 activity will reduce cellular ROS production, leading to reduced probe-ROS interactions and reduced well luminescence. Compounds are considered ‘hits’ and further processed when light emission is blocked >75% 7 than DMSO wells (DMSO and DPI wells are set to 0% and 100% respectively). Compounds are tested in singlicate at a concentration of 10 μM[1].

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

    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
    DMSO 1 mM 4.1440 mL 20.7202 mL 41.4405 mL 103.6012 mL
    5 mM 0.8288 mL 4.1440 mL 8.2881 mL 20.7202 mL
    10 mM 0.4144 mL 2.0720 mL 4.1440 mL 10.3601 mL
    15 mM 0.2763 mL 1.3813 mL 2.7627 mL 6.9067 mL
    20 mM 0.2072 mL 1.0360 mL 2.0720 mL 5.1801 mL
    25 mM 0.1658 mL 0.8288 mL 1.6576 mL 4.1440 mL
    30 mM 0.1381 mL 0.6907 mL 1.3813 mL 3.4534 mL
    40 mM 0.1036 mL 0.5180 mL 1.0360 mL 2.5900 mL
    50 mM 0.0829 mL 0.4144 mL 0.8288 mL 2.0720 mL
    60 mM 0.0691 mL 0.3453 mL 0.6907 mL 1.7267 mL
    80 mM 0.0518 mL 0.2590 mL 0.5180 mL 1.2950 mL
    100 mM 0.0414 mL 0.2072 mL 0.4144 mL 1.0360 mL
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    ML171 Related Classifications

    Help & FAQs
    • 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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