1. GPCR/G Protein
  2. Adenosine Receptor
  3. ZM241385

ZM241385 is a potent, high affinity and selective adenosine A2a receptor (A2AR) antagonist with a Ki value of 1.4 nM.

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

ZM241385 Chemical Structure

ZM241385 Chemical Structure

CAS No. : 139180-30-6

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 73 In-stock
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid
5 mg USD 66 In-stock
10 mg USD 110 In-stock
50 mg USD 396 In-stock
100 mg USD 616 In-stock
200 mg USD 880 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Top Publications Citing Use of Products

    ZM241385 purchased from MedChemExpress. Usage Cited in: Ecotoxicol Environ Saf. 2022 Dec 12;249:114410.  [Abstract]

    ZM241385 (10 μM) significantly decreases the levels of E-cad, increases the N-cad, Vimentin, and α-SMA levels by inhibiting A2aR, in A549 cells.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    ZM241385 is a potent, high affinity and selective adenosine A2a receptor (A2AR) antagonist with a Ki value of 1.4 nM[1][2][3].

    IC50 & Target

    Ki: 1.4 nM (A2AR)[2]

    In Vitro

    ZM241385 (1 μM; 24-48 hours; PC12 cells) treatment reverses the phenomenon that A2AR agonist CGS21680 significantly upregulates A2AR mRNA and protein levels[1].

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

    RT-PCR[1]

    Cell Line: PC12 cells
    Concentration: 1 μM
    Incubation Time: 24 hours
    Result: Suppressed the increased A2AR mRNA levels engendered by CGS21680.

    Western Blot Analysis[1]

    Cell Line: PC12 cells
    Concentration: 1 μM
    Incubation Time: 48 hours
    Result: Decreased A2AR protein levels
    In Vivo

    ZM241385 (0.2 μg/mouse, 0.4 μg/mouse; intraperitoneal injection; every day; for 11 weeks; female C57BL/6 WT mice) treatment decreases tumor volume, activates CD8+ T cells and reduces the frequency of splenic MDSC[4].

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

    Animal Model: Female C57BL/6 WT mice received 4-nitroquinoline-N-oxide[4]
    Dosage: 0.2 μg/mouse, 0.4 μg/mouse
    Administration: Intraperitoneal injection; every day; for 11 weeks
    Result: Decreased tumor volume, activates CD8+ T cells and reduces the frequency of splenic MDSC.
    Molecular Weight

    337.34

    Formula

    C16H15N7O2

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    OC1=CC=C(CCNC2=NC3=NC(C4=CC=CO4)=NN3C(N)=N2)C=C1

    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 : ≥ 30 mg/mL (88.93 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 2.9644 mL 14.8218 mL 29.6437 mL
    5 mM 0.5929 mL 2.9644 mL 5.9287 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: ≥ 2.08 mg/mL (6.17 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    90% (20% SBE-β-CD in Saline)

      Solubility: 2.08 mg/mL (6.17 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 99.26%

    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 2.9644 mL 14.8218 mL 29.6437 mL 74.1092 mL
    5 mM 0.5929 mL 2.9644 mL 5.9287 mL 14.8218 mL
    10 mM 0.2964 mL 1.4822 mL 2.9644 mL 7.4109 mL
    15 mM 0.1976 mL 0.9881 mL 1.9762 mL 4.9406 mL
    20 mM 0.1482 mL 0.7411 mL 1.4822 mL 3.7055 mL
    25 mM 0.1186 mL 0.5929 mL 1.1857 mL 2.9644 mL
    30 mM 0.0988 mL 0.4941 mL 0.9881 mL 2.4703 mL
    40 mM 0.0741 mL 0.3705 mL 0.7411 mL 1.8527 mL
    50 mM 0.0593 mL 0.2964 mL 0.5929 mL 1.4822 mL
    60 mM 0.0494 mL 0.2470 mL 0.4941 mL 1.2352 mL
    80 mM 0.0371 mL 0.1853 mL 0.3705 mL 0.9264 mL
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    ZM241385 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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    Product Name:
    ZM241385
    Cat. No.:
    HY-19532
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