CGS 21680 Hydrochloride
Based on 14 publication(s) in Google Scholar
CGS 21680 Hydrochloride is a selective adenosine A2A receptor agonist with a Ki of 27 nM.
For research use only. We do not sell to patients.
- Purity: 99.70%
- CAS No.: 124431-80-7
- Formula: C23H30ClN7O6
- Molecular Weight:535.98
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) CGS 21680 Hydrochloride
More- Nature. 2026 Jan;649(8096):423-431. [Abstract]
- J Neuroinflammation. 2022 Feb 18;19(1):52. [Abstract]
- Cell Death Dis. 2020 Mar 23;11(3):202. [Abstract]
- Acta Pharmacol Sin. 2025 May;46(5):1177-1189. [Abstract]
- Cell Mol Gastroenterol Hepatol. 2025 May 21:101539. [Abstract]
- Ecotoxicol Environ Saf. 2023 Jan 1:249:114410. [Abstract]
- J Cell Mol Med. 2025 Mar;29(5):e70458. [Abstract]
- Neurochem Int. 2021 May:145:104983. [Abstract]
- Eur J Med Res. 2024 Aug 27;29(1):433. [Abstract]
- Iran J Basic Med Sci. 2021 Oct;24(10):1380-1387. [Abstract]
- Placenta. 2025 Dec:172:150-158. [Abstract]
- bioRxiv. 2026 Jan 6:2026.01.06.697936. [Abstract]
- Research Square Print. December 13th, 2022.
- Research Square Preprint. 2021 Aug.
Customer Validation & Images
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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Flow Cytometry
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Others
All Adenosine Receptor Isoforms
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Biological Activity
Ki: 27 nM (Adenosine A2A receptor)[5]
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 124431-80-7
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Appearance Solid
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Molecular Weight 535.98
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Formula C23H30ClN7O6
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Color White to off-white
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SMILES
O=C(O)CCC1=CC=C(CCNC2=NC3=C(N=CN3[C@H]4[C@H](O)[C@H](O)[C@@H](C(NCC)=O)O4)C(N)=N2)C=C1.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications (14)
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Journal Impact Factor
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Most Recent
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Nature
2026 Jan;649(8096):423-431. PMID: 41193806
CGS 21680 Hydrochloride 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 Hydrochloride 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 Hydrochloride 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.
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J Neuroinflammation
Choroid plexus-selective inactivation of adenosine A2A receptors protects against T cell infiltration and experimental autoimmune encephalomyelitis. [Abstract]2022 Feb 18;19(1):52. PMID: 35180864 -
Cell Death Dis
CD73 promotes tumor metastasis by modulating RICS/RhoA signaling and EMT in gastric cancer. [Abstract]2020 Mar 23;11(3):202. PMID: 32205841 -
Acta Pharmacol Sin
Compound 38, a novel potent and selective antagonist of adenosine A2A receptor, enhances arousal in mice. [Abstract]2025 May;46(5):1177-1189. PMID: 39779967 -
Cell Mol Gastroenterol Hepatol
2025 May 21:101539. PMID: 40409684
CGS 21680 Hydrochloride 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).
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Ecotoxicol Environ Saf
A2aR inhibits fibrosis and the EMT process in silicosis by regulating Wnt/β-catenin pathway. [Abstract]2023 Jan 1:249:114410. PMID: 36516619
CGS 21680 Hydrochloride 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.
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J Cell Mol Med
Macrophage A2aR Alleviates LPS-Induced Vascular Endothelial Injury and Inflammation via Inhibiting M1 Polarisation and Oxidative Stress. [Abstract]2025 Mar;29(5):e70458. PMID: 40045158
CGS 21680 Hydrochloride 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 Hydrochloride 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 Hydrochloride 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 Hydrochloride 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).
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Neurochem Int
Electroacupuncture improves neuronal plasticity through the A2AR/cAMP/PKA signaling pathway in SNL rats. [Abstract]2021 May:145:104983. PMID: 33577869 -
Eur J Med Res
A2AR regulate inflammation through PKA/NF-κB signaling pathways in intervertebral disc degeneration. [Abstract]2024 Aug 27;29(1):433. PMID: 39192377 -
Iran J Basic Med Sci
A2 adenosine receptor contributes to the development of cow's milk protein allergy via regulating regulatory T cells. [Abstract]2021 Oct;24(10):1380-1387. PMID: 35096296 -
Placenta
Adenosine promotes trophoblast proliferation without inducing differentiation or apoptosis. [Abstract]2025 Dec:172:150-158. PMID: 41240505 -
bioRxiv
Host GPCR-cAMP signaling balances Gαs and Gαi activity to control intracellular Brucella infection. [Abstract]2026 Jan 6:2026.01.06.697936. PMID: 41542404 -
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Solvent & Solubility
DMSO : ≥ 20 mg/mL (37.31 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
* "≥" means soluble, but saturation unknown.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.66 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.66 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.
Please enter the basic information of animal experiments:
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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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Bao R, et al. Adenosine and the adenosine A2A receptor agonist, CGS21680, upregulate CD39 and CD73 expression through E2F-1 and CREB in regulatory T cells isolated from septic mice. Int J Mol Med. 2016 Sep;38(3):969-75. [Content Brief]
[2]. Komaki S, et al. Trk and cAMP-dependent survival activity of adenosine A(2A) agonist CGS21680 on rat motoneurons in culture. Neurosci Lett. 2012 Jul 26;522(1):21-4. [Content Brief]
[3]. Zhang M, et al. Activation of the adenosine A2A receptor exacerbates experimental autoimmune neuritis in Lewis rats in association with enhanced humoral immunity. J Neuroimmunol. 2016 Apr 15;293:129-36. [Content Brief]
[5]. Melani A, et al. Low doses of the selective adenosine A2A receptor agonist CGS21680 are protective in a rat model of transient cerebral ischemia. Brain Res. 2014 Mar 10;1551:59-72. [Content Brief]
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 (sealed storage, away from moisture). 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 | 1.8657 mL | 9.3287 mL | 18.6574 mL | 46.6435 mL |
| 5 mM | 0.3731 mL | 1.8657 mL | 3.7315 mL | 9.3287 mL | |
| 10 mM | 0.1866 mL | 0.9329 mL | 1.8657 mL | 4.6644 mL | |
| 15 mM | 0.1244 mL | 0.6219 mL | 1.2438 mL | 3.1096 mL | |
| 20 mM | 0.0933 mL | 0.4664 mL | 0.9329 mL | 2.3322 mL | |
| 25 mM | 0.0746 mL | 0.3731 mL | 0.7463 mL | 1.8657 mL | |
| 30 mM | 0.0622 mL | 0.3110 mL | 0.6219 mL | 1.5548 mL |
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