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

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

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

CAS No. : 120225-54-9

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10 mM * 1 mL in DMSO
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Customer Review

Based on 14 publication(s) in Google Scholar

Other Forms of CGS 21680:

CGS 21680 Related Antibodies

Top Publications Citing Use of Products

    CGS 21680 purchased from MedChemExpress. Usage Cited in: Nature. 2026 Jan;649(8096):423-431.  [Abstract]

    Immobility time in forced swimming test 30 minutes after intraperitoneal (i.p.) injection of an A1 receptor agonist (CHA; 0.1 mg/kg) or an A2A receptor agonist (CGS 21680 Hydrochloride; 0.1 mg/kg) in chronic restraint stress (CRS) mice.

    CGS 21680 purchased from MedChemExpress. Usage Cited in: Nature. 2026 Jan;649(8096):423-431.  [Abstract]

    Twenty-four hours after intraperitoneal injection of CHA or CGS21680 (CGS 21680 Hydrochloride; 0.1 mg/kg) into CRS mice, immobility time and sucrose preference in the forced swimming test were measured.

    CGS 21680 purchased from MedChemExpress. Usage Cited in: Nature. 2026 Jan;649(8096):423-431.  [Abstract]

    Concentrations of CHA and CGS 21680 Hydrochloride in serum (top) and brain tissue (bottom) at 30 min and 24 h after i.p. injection, measured by LC-MS. Data are mean ± s.e.m.

    CGS 21680 purchased from MedChemExpress. Usage Cited in: Cell Mol Gastroenterol Hepatol. 2025 May 21:101539.  [Abstract]

    Percentage quantification of ASCs after 3 days of treatment with the A2aR agonist CGS 21680 Hydrochloride (1 μM) with or without Inosine (250 μM).

    CGS 21680 purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2025 Mar;29(5):e70458.  [Abstract]

    Schematic illustration showed that CGS 21680 Hydrochloride (1 mg/kg) or dimethyl sulfoxide (DMSO) was instilled combined with LPS (5 mg/kg) challenge for 24 h.

    CGS 21680 purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2025 Mar;29(5):e70458.  [Abstract]

    WT and Mac‐A2aR‐KO mice were treated with LPS (5 mg/kg) and CGS 21680 Hydrochloride (1 mg/kg) or PBS for 24 h. Assessment of kidney oedema (n = 3).

    CGS 21680 purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2025 Mar;29(5):e70458.  [Abstract]

    Intracellular total ROS was detected in PMA‐differentiated THP‐1 cells treated with vehicle, CGS 21680 Hydrochloride (10 nM), LPS (1 μg/mL) or LPS after 30 min CGS 21680 Hydrochloride pretreatment (n = 3).

    CGS 21680 purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2025 Mar;29(5):e70458.  [Abstract]

    Intracellular total ROS was detected in PMA‐differentiated THP‐1 cells treated with vehicle, LPS (100 μg/mL) and interferon‐gamma (IFN‐γ) (20 ng/mL) with or without 30 min CGS 21680 Hydrochloride pretreatment before; interleukin (IL)‐4 (20 ng/mL) and IL‐13 (20 ng/mL) with or without 30 min CGS 21680 Hydrochloride pretreatment before (n = 3).

    CGS 21680 purchased from MedChemExpress. Usage Cited in: Ecotoxicol Environ Saf. 2023 Jan 1:249:114410.  [Abstract]

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

    View All Adenosine Receptor Isoform Specific Products:

    View All Isoforms
    Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    IC50 & Target

    Ki: 27 nM (Adenosine A2A receptor) [5]
    Cellular Effect
    Cell Line Type Value Description References
    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]
    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]
    Neutrophil IC50
    47 nM
    Compound: 1, CGS-21680
    Inhibition of fLMP-induced super oxide production in human neutrophils
    Inhibition of fLMP-induced super oxide production in human neutrophils
    		[PMID: 18243699]
    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]
    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].

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

    CGS 21680 Related Antibodies
    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].

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

    499.52

    Formula

    C23H29N7O6
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(CCC1=CC=C(C=C1)CCNC2=NC3=C(C(N)=N2)N=CN3[C@H]4[C@@H]([C@@H]([C@H](O4)C(NCC)=O)O)O)O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (100.10 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 2.0019 mL 10.0096 mL 20.0192 mL
    5 mM 0.4004 mL 2.0019 mL 4.0038 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
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    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

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    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: ≥ 2.5 mg/mL (5.00 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.00 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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
    References
    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.
    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.0019 mL 10.0096 mL 20.0192 mL 50.0480 mL
    5 mM 0.4004 mL 2.0019 mL 4.0038 mL 10.0096 mL
    10 mM 0.2002 mL 1.0010 mL 2.0019 mL 5.0048 mL
    15 mM 0.1335 mL 0.6673 mL 1.3346 mL 3.3365 mL
    20 mM 0.1001 mL 0.5005 mL 1.0010 mL 2.5024 mL
    25 mM 0.0801 mL 0.4004 mL 0.8008 mL 2.0019 mL
    30 mM 0.0667 mL 0.3337 mL 0.6673 mL 1.6683 mL
    40 mM 0.0500 mL 0.2502 mL 0.5005 mL 1.2512 mL
    50 mM 0.0400 mL 0.2002 mL 0.4004 mL 1.0010 mL
    60 mM 0.0334 mL 0.1668 mL 0.3337 mL 0.8341 mL
    80 mM 0.0250 mL 0.1251 mL 0.2502 mL 0.6256 mL
    100 mM 0.0200 mL 0.1001 mL 0.2002 mL 0.5005 mL
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    CGS 21680 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.

    Keywords:

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

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