2. GPCR/G Protein
  3. Adenosine Receptor
  4. CGS 21680

CGS 21680 是一种选择性的 adenosine A2A receptor 特异性激动剂，Ki 值为 27 nM。

该游离形式化合物不稳定，推荐具有相同生物学活性的稳定盐形式 CGS 21680 Hydrochloride。

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CGS 21680 Chemical Structure

CGS 21680 Chemical Structure

CAS No. : 120225-54-9

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CGS 21680 的其他形式现货产品:

Other Forms of CGS 21680:

CGS 21680 相关抗体

Top Publications Citing Use of Products

    CGS 21680 purchased from MCE. Usage Cited in: Ecotoxicol Environ Saf. 2022 Dec 12;249:114410.  [Abstract]

    CGS21680 (10 μM) elevates the expression level of A2aR protein in A549 cells.

    查看 Adenosine Receptor 亚型特异性产品:

    查看所有亚型
    Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    CGS 21680 is a selective adenosine A2A receptor agonist, with a Ki of 27 nM.

    IC50 & Target

    Ki: 27 nM (Adenosine A2A receptor) [5]
    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    CHO EC50
    > 10000 nM
    Compound: 2, CGS21680
    Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
    Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
    		[PMID: 25780876]
    CHO EC50
    > 10000 nM
    Compound: CGS-21680
    Agonist activity at human adenosine A1 receptor expressed in CHO cells by GTPPgammaS binding assay
    Agonist activity at human adenosine A1 receptor expressed in CHO cells by GTPPgammaS binding assay
    		[PMID: 20031406]
    CHO EC50
    > 10000 nM
    Compound: CGS-21680
    Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as effect on cAMP production by luciferase reporter gene assay
    Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as effect on cAMP production by luciferase reporter gene assay
    		[PMID: 20031406]
    CHO EC50
    18.47 nM
    Compound: 2, CGS21680
    Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
    Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
    		[PMID: 25780876]
    CHO EC50
    2.12 nM
    Compound: 1, CGS 21680
    Agonist activity at human adenosine A2a receptor expressed in CHO cells assessed as stimulation of cAMP formation after 24 hrs
    Agonist activity at human adenosine A2a receptor expressed in CHO cells assessed as stimulation of cAMP formation after 24 hrs
    		[PMID: 25221664]
    CHO EC50
    613 nM
    Compound: CGS-21680
    Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
    Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay
    		[PMID: 20031406]
    PBMC IC50
    58 nM
    Compound: CGS-21680
    Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha production after 20 hrs by ELISA
    Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha production after 20 hrs by ELISA
    		[PMID: 20031406]
    PBMC IC50
    83 nM
    Compound: CGS-21680
    Antiinflammatory activity in rat PBMC assessed as inhibition of LPS-induced TNFalpha production after 20 hrs by ELISA
    Antiinflammatory activity in rat PBMC assessed as inhibition of LPS-induced TNFalpha production after 20 hrs by ELISA
    		[PMID: 20031406]
    体外研究
    (In Vitro)

    CGS21680 significantly upregulates CD39 and CD73 expression. CGS21680 accelerates the adenosine triphosphate (ATP) hydrolysis and adenosine generation[1]. CGS21680 (10 nM) alone shows only small survival activity, but the activity is significantly enhanced by the addition of a phosphodiesterase inhibitor, IBMX. The survival activity of CGS21680 on cultured motoneurons is exerted by mixed effects of the adenylate cyclase-cAMP-PKA pathway and the transactivation of neurotrophin receptors[4].

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

    CGS 21680 相关抗体:
    体内研究
    (In Vivo)

    CGS21680 (1 mg/kg/i.p.) intervention promotes the development of EAN. CGS21680 exacerbates experimental autoimmune neuritis in Lewis rats induced with bovine peripheral myelin. The exacerbation is accompanied with reduced CD4+ Foxp3+ T cells, increased CD4+ CXCR5+ T cells, B cells, dendritic cells and antigen-specific autoantibodies, which is possibly due to the inhibition of IL-2 induced by CGS21680[2]. CGS21680 (0.1 mg/kg, i.p.) transiently increases heart frequency but does not modify blood pressure of rat, and does not modify either heart frequency or blood pressure at 0.01 mg/kg. Following transient MCAo, CGS21680 at both doses protects from neurological deficit from the first day up to 7 days thereafter. At this time, it has reduced microgliosis, astrogliosis and improved myelin organization in the striatum and cytoarchitecture of the ischemic cortex and striatum. Two days after transient MCAo, CGS21680 has reduced the number of infiltrated granulocytes into the ischemic tissue[3].

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

    499.52

    Formula

    C23H29N7O6
    CAS 号
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.
    纯度 & 产品资料
    参考文献
    Cell Assay
    [2]

    10×106 MNCs from each group are re-suspended in 2 mL RPMI 1640. Cell suspensions are added with carboxy-fluorescein diacetate, succinimidyl ester (CFSE, final concentration 2.5 μM) and thoroughly mixed. After incubation in the dark for 15 min at 37°C, the staining process is quenched by adding 10 mL ice-cold complete RPMI 1640 (containing 10% FBS) and incubated on ice for 5 min. Then cells are washed twice with RPMI 1640. Cell pellets are re-suspended in complete RPMI 1640 (containing 10% FBS). The stained MNCs (1×106 cells/mL, 1 mL/well) are cultured in triplicates in 24-well culture plates in the dark at 37°C. Each well is supplied with 50 μL of Concanavalin A (ConA, final concentration 5 μg/mL) or 50 μL of P0 peptide (final concentration 10 μg/mL). 72 h later, cells are collected and stained with PE-labeled anti-rat CD4 antibody for 30 min at 4°C. Finally, cells are analyzed with a flow cytometer.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Female Lewis rats aged 6-8 weeks (body weight, 140-160 g) are housed under specific pathogen-free conditions in the local animal facility with free access to water and food. Administration of CGS21680 (at a dose of 1 mg/kg in PBS) starts on day 5 p.i. Rats in experimental group are injected with CGS21680 intraperitoneally (i.p.) every two days until the end of the experiments. Rats in control group are given equal volume of PBS in the same way. The doses (1 mg/kg/i.p.) and the treatment regimen (every two days, start on day 5 p.i.) are determined.

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

    CGS 21680 相关分类

    • 摩尔计算器

    • 稀释计算器

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    × = ×
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    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:

    CGS 21680120225-54-9CGS21680CGS-21680Adenosine ReceptorP1 receptorInhibitorinhibitorinhibit

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    产品名称：
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    目录号：
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