2. GPCR/G Protein
  3. Adenosine Receptor
  4. BAY 60-6583

BAY 60-6583 is a potent and high-affinity agonist of adenosine A2B receptor (EC50=3 nM) over A1, A2A, and A3 receptors. BAY 60-6583 binds to mouse, rabbit, and dog A2BAR with Ki values of 750 nM, 340 nM and 330 nM, respectively. BAY 60-6583 has a cardioprotective effect in a myocardial ischemia model.

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CAS 番号 : 910487-58-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 108 在庫あり
Solution
10 mM * 1 mL in DMSO USD 108 在庫あり
Solid
5 mg $99 在庫あり
10 mg $160 在庫あり
25 mg $337 在庫あり
50 mg $506 在庫あり
100 mg $760 在庫あり
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カスタマーレビュー

Based on 7 publication(s) in Google Scholar

Other Forms of BAY 60-6583:

BAY 60-6583 関連抗体

Top Publications Citing Use of Products

    BAY 60-6583 purchased from MedChemExpress. Usage Cited in: J Inflamm Res. 2025 Mar 6:18:3283-3294.  [Abstract]

    The procedure of mice experiments. Intervention group: CA mice were interpertional with A1R agonist (CCPA), A2AR agonist (GCS21680) or antagonist (KW6002), A2BR agonist (BAY 60–6583) and A3R agonist (2-CI-IB-MECA).

    BAY 60-6583 purchased from MedChemExpress. Usage Cited in: PeerJ. 2023 Aug 30:11:e15922.

    CAL27 cells were treated with BAY60-6583 (A2BR agonist) for 24 h. Real-time quantitative reverse transcription PCR assay showing the mRNA levels of PD-L1 in CAL27 cells after BAY 60-6583 treatment.

    BAY 60-6583 purchased from MedChemExpress. Usage Cited in: PeerJ. 2023 Aug 30:11:e15922.

    CAL27 cells were treated with BAY60-6583 (A2BR agonist) for 24 h. Flow cytometry assay showing the surface localization of PD-L1 in CAL27 cells after BAY60-6583 treatment.

    BAY 60-6583 purchased from MedChemExpress. Usage Cited in: PeerJ. 2023 Aug 30:11:e15922.

    CAL27 cells were treated with BAY60-6583 (A2BR agonist) for 24 h. The mean fluorescence intensity of PD-L1 in CAL27 cells after BAY60-6583 treatment.

    BAY 60-6583 purchased from MedChemExpress. Usage Cited in: PeerJ. 2023 Aug 30:11:e15922.

    CAL27 cells were treated with BAY60-6583 (A2BR agonist) for 24 h. Western blot assay showing the levels of pNF-κ Bp65 after BAY60-6583 treatment.

    BAY 60-6583 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2022 Dec 23;8(51):eadd3709.  [Abstract]

    The potency of BAY60-6583 on the pocket mutations of A2AR.

    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

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    製品説明

    BAY 60-6583 is a potent and high-affinity agonist of adenosine A2B receptor (EC50=3 nM) over A1, A2A, and A3 receptors. BAY 60-6583 binds to mouse, rabbit, and dog A2BAR with Ki values of 750 nM, 340 nM and 330 nM, respectively. BAY 60-6583 has a cardioprotective effect in a myocardial ischemia model[1][5].

    体外実験

    BAY 60-6583 exhibits EC50 values for receptor activation >10,000 nM for both A1 and A2A AR and 3 nM for A2B AR subtype in CHO cells expressing recombinant human A1, A2A or A2B ARs[1].
    BAY 60-6583 (0-10 μM) exhibits the maximum agonist effect of BAY in the absence of siRNA is 68 %, which is significantly different from that in the presence of 5, 50 and 500 nM siRNA (54%, 48% and 36%, respectively). It exhibits EC50 values of BAY in the absence and presence siRNA with 98±22, 102±17, 127±31 and 93±19 nM, respectively, in T24 cells[3].
    BAY 60-6583 (5 μM; 24 hours) increases the accumulation of cells at the G1 phase with a decrease in G2/M phase in RAW264.7 preosteoclasts[4].
    BAY 60-6583 (5 μM; 24 hours) specifically inhibits the activation of Akt by M-CSF, whereas M-CSF-induced ERK1/2 activation is not affected by BAY 60-6583 treatment in RAW264.7 preosteoclasts[4].

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

    BAY 60-6583 関連抗体

    Cell Cycle Analysis[4]

    Cell Line: RAW264.7 preosteoclasts
    Concentration: 5 μM
    Incubation Time: 48 hours
    Result: Caused an arrest of cells at the G1 phase.

    Western Blot Analysis[4]

    Cell Line: RAW264.7 preosteoclasts
    Concentration: 5 μM
    Incubation Time: 48 hours
    Result: Exhibited an inhibition of M-CSF-mediated Akt activation and resulted in the decrease of osteoclast proliferation.
    体内実験

    BAY 60-6583 (intravenous injection; 100 mcg/kg) reduces the infarction area just prior to reperfusion in ischaemic rabbit hearts[1].
    BAY 60-6583 (intraperitoneal injection; 2 mg/kg) attenuates LPS-induced lung injury, pre-treatment with this compound can significantly decrease LPS-increased IL-6 levels in WT-mice, In contrast, BAY 60-6583 treatment is ineffective in abrogating these inflammatory parameters in A2BAR mice[2].
    BAY 60-6583 (intratumoral administration) causes a significant increase in tumor-infiltrating MDSCs, it does not affect neither their ability to suppress T-cell proliferation nor their degree of maturation, it also stimulates the production of IL-10 and CCL2 in the tumor tissue[5].

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

    Animal Model:  A2BAR−/−  mice on a C57BL/6J mice[1]
    Dosage: 2 mg/kg
    Administration: Intraperitoneal injection; 2 mg/kg
    Result: Demonstrated attenuation of lung inflammation and pulmonary edema in wild-type but not in gene-targeted mice for the A2BAR.
    分子量

    379.44

    分子式

    C19H17N5O2S
    CAS 番号
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=C(N)CSC1=NC(N)=C(C#N)C(C2=CC=C(OCC3CC3)C=C2)=C1C#N
    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 (263.55 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 2.6355 mL 13.1773 mL 26.3546 mL
    5 mM 0.5271 mL 2.6355 mL 5.2709 mL
    10 mM 0.2635 mL 1.3177 mL 2.6355 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

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    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: ≥ 4.17 mg/mL (10.99 mM); Clear solution

      This protocol yields a clear solution of ≥ 4.17 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (41.7 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: ≥ 4.17 mg/mL (10.99 mM); Clear solution

      This protocol yields a clear solution of ≥ 4.17 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 (41.7 mg/mL) to 900 μL Corn oil, and mix evenly.

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    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: 99.93%

    COA (247 KB) LCMS (93 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 2.6355 mL 13.1773 mL 26.3546 mL 65.8866 mL
    5 mM 0.5271 mL 2.6355 mL 5.2709 mL 13.1773 mL
    10 mM 0.2635 mL 1.3177 mL 2.6355 mL 6.5887 mL
    15 mM 0.1757 mL 0.8785 mL 1.7570 mL 4.3924 mL
    20 mM 0.1318 mL 0.6589 mL 1.3177 mL 3.2943 mL
    25 mM 0.1054 mL 0.5271 mL 1.0542 mL 2.6355 mL
    30 mM 0.0878 mL 0.4392 mL 0.8785 mL 2.1962 mL
    40 mM 0.0659 mL 0.3294 mL 0.6589 mL 1.6472 mL
    50 mM 0.0527 mL 0.2635 mL 0.5271 mL 1.3177 mL
    60 mM 0.0439 mL 0.2196 mL 0.4392 mL 1.0981 mL
    80 mM 0.0329 mL 0.1647 mL 0.3294 mL 0.8236 mL
    100 mM 0.0264 mL 0.1318 mL 0.2635 mL 0.6589 mL
    • No file chosen (Maximum size is: 1024 Kb)
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    BAY 60-6583 Related Classifications

    • Molarity Calculator

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    一般には略語で表示されます：C1V1 = C2V2

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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.

    Keywords:

    BAY 60-6583910487-58-0Adenosine ReceptorP1 receptorAcute Lung Injurypulmonary edematype 2 diabetesobesitymyocardial ischemiaInhibitorinhibitorinhibit

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    製品番号:
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