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

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

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CAS 番号 : 139180-30-6

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Solid
5 mg $66 在庫あり
10 mg $110 在庫あり
25 mg $242 在庫あり
50 mg $396 在庫あり
100 mg $550 在庫あり
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カスタマーレビュー

Based on 14 publication(s) in Google Scholar

Other Forms of ZM241385:

ZM241385 関連抗体

Top Publications Citing Use of Products

    ZM241385 purchased from MedChemExpress. Usage Cited in: ACS Nano. 2025 Oct 21;19(41):36353-36372.  [Abstract]

    Intracellular cAMP concentrations in CD8+ T cells after various treatments. Pretreatment with ZM241385 (10 μM; 12 h) can inhibit effects of SBRT by reducing cAMP levels.

    ZM241385 purchased from MedChemExpress. Usage Cited in: ACS Nano. 2025 Oct 21;19(41):36353-36372.  [Abstract]

    Proportion of pCREB+CD8+ T cells after various treatments. Pretreatment with ZM241385 (10 μM; 12 h) can inhibit effects of SBRT by reducing CREB phosphorylation.

    ZM241385 purchased from MedChemExpress. Usage Cited in: Mater Today. 2024 Apr 26.

    Bath application of ZM241385 (1 μM, 10 min) significantly inhibited seizure-like discharges in the brain slices of TLE participants.

    ZM241385 purchased from MedChemExpress. Usage Cited in: Mater Today. 2024 Apr 26.

    In vivo EEG recording of epileptic mice treated with vehicle or ZM241385 (2 mg/kg; i.p.; every other day for 3 weeks). The number of seizures per day and seizure duration were analyzed. The A2AR antagonist ZM241385 markedly reduced KA-induced seizure activities in mice.

    ZM241385 purchased from MedChemExpress. Usage Cited in: Nat Neurosci. 2023 Apr;26(4):542-554.  [Abstract]

    Representative flow cytometric analysis, and quantitative of divided T cells after various treatments. ZM241385 reversed the inhibition effect of adenosine on T cells.

    ZM241385 purchased from MedChemExpress. Usage Cited in: Ecotoxicol Environ Saf. 2023 Jan 1:249:114410.  [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.

    Adenosine Receptor アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

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    • 純度とドキュメンテーション

    • 参考文献

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    製品説明

    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[2] [1]

    A2AR

    1.4 nM (Ki)

    Cellular Effect
    Cell Line Type Value Description References
    CHO EC50
    > 100000 1
    Compound: 1, ZM 241385
    Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
    Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
    		[PMID: 25490054]
    CHO IC50
    0.678 1
    Compound: 1; ZM 241385
    Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
    Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
    		[PMID: 27933962]
    CHO IC50
    0.678 1
    Compound: 1; ZM 241385
    Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
    Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
    		[PMID: 27933962]
    CHO EC50
    >100 3
    Compound: 1, ZM 241385
    Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
    Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
    		[PMID: 25490054]
    CHO IC50
    1.45 1
    Compound: 1; ZM 241385
    Inverse agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
    Inverse agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
    		[PMID: 27933962]
    CHO IC50
    1.45 1
    Compound: 1; ZM 241385
    Inverse agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
    Inverse agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
    		[PMID: 27933962]
    CHO IC50
    33 1
    Compound: 1, ZM 241385
    Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
    Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
    		[PMID: 25490054]
    CHO IC50
    33 1
    Compound: 1, ZM 241385
    Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
    Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
    		[PMID: 25490054]
    CHO IC50
    42 1
    Compound: 5, ZM 241385
    Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
    Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
    		[PMID: 23602401]
    CHO IC50
    42 1
    Compound: 5, ZM 241385
    Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
    Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
    		[PMID: 23602401]
    CHO EC50
    > 100000 1
    Compound: 1, ZM 241385
    Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
    Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
    		[PMID: 25490054]
    CHO IC50
    48 1
    Compound: 1; ZM 241385
    Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
    Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
    		[PMID: 27933962]
    CHO IC50
    48 1
    Compound: 1; ZM 241385
    Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
    Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
    		[PMID: 27933962]
    CHO IC50
    0.678 1
    Compound: 1; ZM 241385
    Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
    Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
    		[PMID: 27933962]
    CHO IC50
    1.45 1
    Compound: 1; ZM 241385
    Inverse agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
    Inverse agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
    		[PMID: 27933962]
    CHO IC50
    33 1
    Compound: 1, ZM 241385
    Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
    Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
    		[PMID: 25490054]
    CHO IC50
    42 1
    Compound: 5, ZM 241385
    Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
    Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
    		[PMID: 23602401]
    CHO IC50
    48 1
    Compound: 1; ZM 241385
    Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
    Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
    		[PMID: 27933962]
    体外実験

    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.

    ZM241385 関連抗体

    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
    体内実験

    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.
    分子量

    337.34

    分子式

    C16H15N7O2
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 100 mg/mL (296.44 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 2.9644 mL 14.8218 mL 29.6437 mL
    5 mM 0.5929 mL 2.9644 mL 5.9287 mL
    10 mM 0.2964 mL 1.4822 mL 2.9644 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.

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    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

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    体内:

    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:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 6.25 mg/mL (18.53 mM); Clear solution

    • Protocol 2

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

      Solubility: ≥ 5 mg/mL (14.82 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  50% PEG300    50% Saline

      Solubility: 12.5 mg/mL (37.05 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
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    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.
    純度とドキュメンテーション

    純度: 99.45%

    COA (245 KB) HNMR (136 KB) RP-HPLC (138 KB) LCMS (105 KB)

    取扱説明書 (2659 KB)
    参考文献

    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
    100 mM 0.0296 mL 0.1482 mL 0.2964 mL 0.7411 mL
    • No file chosen (Maximum size is: 1024 Kb)
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    ZM241385 Related Classifications

    • Molarity Calculator

    • Dilution Calculator

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    The dilution calculator equation

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    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.

    Keywords:

    ZM241385139180-30-6ZM 241385ZM-241385Adenosine ReceptorP1 receptorInhibitorinhibitorinhibit

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    製品名:
    ZM241385
    製品番号:
    HY-19532
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