RU.521 [2262452-06-0]

Referentie HY-114180-10mg

Formaat : 10mg

Merk : MedChemExpress

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RU.521 (RU320521) is a potent and selective cyclic GMP-AMP synthase (cGAS) inhibitor and inhibits cGAS-mediated interferon upregulation. RU.521 suppresses dsDNA-activated reporter activity with an IC50 of 0.7 μM. RU.521 reduces constitutive expression of interferon in macrophages from a mouse model of Aicardi-Goutières syndrome (AGS).

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RU.521 Chemical Structure

RU.521 Chemical Structure

CAS No. : 2262452-06-0

This product is a controlled substance and not for sale in your territory.

Based on 27 publication(s) in Google Scholar

    RU.521 purchased from MedChemExpress. Usage Cited in: Toxicol Lett. 2022 Nov 8;S0378-4274(22)01779-9.  [Abstract]

    RU.521 (2.4 μM) significantly reduces the elevation of cGAS and STING triggered by ZnONPs in BEAS-2B cells.
    Description

    RU.521 (RU320521) is a potent and selective cyclic GMP-AMP synthase (cGAS) inhibitor and inhibits cGAS-mediated interferon upregulation. RU.521 suppresses dsDNA-activated reporter activity with an IC50 of 0.7 μM. RU.521 reduces constitutive expression of interferon in macrophages from a mouse model of Aicardi-Goutières syndrome (AGS)[1].

    IC50 & Target

    IC50: 0.7 μM (dsDNA)[1]

    In Vitro

    RU.521 (0.1 nM-1000 μM; 72 h) suppresses dsDNA-induced signaling in macrophage cells[1].
    RU.521(0-100 μM; 24 h) selectively inhibits cGAS-mediated signaling[1].

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

    In Vivo

    RU.521 (5 mg/kg ; i.p. once) reduces symptoms from sepsis in mice[2].

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

    Animal Model: Male 8-week-old male mice with LPS injection[2]
    Dosage: 5 mg/kg
    Administration: Intraperitoneal injection; 5 mg/kg once
    Result: Increased cardiac function and reduced the inflammatory responses, oxidative stress and apoptosis in hearts of mice.
    Masse moléculaire

    415.23

    Formule

    C19H12Cl2N4O3

    CAS No.

    2262452-06-0

    Appearance

    Solid

    Color

    Off-white to yellow

    SMILES

    O=C1OC(C2=C(O)N(C3=NC4=CC=C(Cl)C(Cl)=C4N3)N=C2C)C5=C1C=CC=C5

    Livraison

    Room temperature in continental US; may vary elsewhere.

    Stockage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvant et solubilité
    In Vitro: 

    DMSO : 83.33 mg/mL (200.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4083 mL 12.0415 mL 24.0830 mL
    5 mM 0.4817 mL 2.4083 mL 4.8166 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.

    • Calculateur de molarité

    • Calculateur de dilution

    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: ≥ 2.08 mg/mL (5.01 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (5.01 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
    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.
    Pureté et documentation

    Purity: 99.89%

    Références
    • [1]. Vincent J, et al. Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice. Nat Commun. 2017 Sep 29;8(1):750.  [Content Brief]

      [2]. Xu Q, et al. Small molecule inhibition of cyclic GMP-AMP synthase ameliorates sepsis-induced cardiac dysfunction in mice. Life Sci. 2020 Nov 1;260:118315.  [Content Brief]

    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 2.4083 mL 12.0415 mL 24.0830 mL 60.2076 mL
    5 mM 0.4817 mL 2.4083 mL 4.8166 mL 12.0415 mL
    10 mM 0.2408 mL 1.2042 mL 2.4083 mL 6.0208 mL
    15 mM 0.1606 mL 0.8028 mL 1.6055 mL 4.0138 mL
    20 mM 0.1204 mL 0.6021 mL 1.2042 mL 3.0104 mL
    25 mM 0.0963 mL 0.4817 mL 0.9633 mL 2.4083 mL
    30 mM 0.0803 mL 0.4014 mL 0.8028 mL 2.0069 mL
    40 mM 0.0602 mL 0.3010 mL 0.6021 mL 1.5052 mL
    50 mM 0.0482 mL 0.2408 mL 0.4817 mL 1.2042 mL
    60 mM 0.0401 mL 0.2007 mL 0.4014 mL 1.0035 mL
    80 mM 0.0301 mL 0.1505 mL 0.3010 mL 0.7526 mL
    100 mM 0.0241 mL 0.1204 mL 0.2408 mL 0.6021 mL
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    RU.521 Related Classifications

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    Keywords:

    RU.5212262452-06-0RU320521RU 320521RU-320521Cyclic GMP-AMP SynthasecGASsignaling pathwayoxidative stressinflammatoryInhibitorinhibitorinhibit

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