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CGS 21680

14 Cited Publications

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Based on 14 publication(s) in Google Scholar

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

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Reinheit: 99.88%
CAS. Nr.: 120225-54-9
Formel: C₂₃H₂₉N₇O₆
Molecular Weight:499.52

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

CGS 21680 Chemical Structure

CAS. Nr.: 120225-54-9

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (14)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

IC₅₀ & Target

Ki: 27 nM (Adenosine A2A receptor) ^[5]

Alle Adenosine Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
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	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: 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	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	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	>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]
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.

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.

Chemical Information

CAS. Nr. 120225-54-9
Appearance Solid
Molecular Weight 499.52
Formel C₂₃H₂₉N₇O₆
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (14)

All Flow CytometryOthersIn Vivo Efficacy StudyBio/Physico-chemical AssayWB

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Journal Impact Factor

Nature

Adenosine signalling drives antidepressant actions of ketamine and ECT. [Abstract]

2026 Jan;649(8096):423-431. PMID: 41193806

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.
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
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
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

Extracellular Inosine Induces Anergy in B Cells to Alleviate Autoimmune Hepatitis. [Abstract]

2025 May 21:101539. PMID: 40409684

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

CGS21680 (10 μM) elevates the expression level of A_2aR protein in A549 cells.
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
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 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).
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
Research Square Print

December 13th, 2022.
Research Square Preprint

2021 Aug.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0019 mL

10.0096 mL

20.0192 mL

5 mM

0.4004 mL

2.0019 mL

4.0038 mL

10 mM

0.2002 mL

1.0010 mL

2.0019 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

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.

MedChemExpress (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.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]. Rosaria Volpini, et al. Adenosine receptor agonists: synthesis and binding affinity of 2-(aryl)alkylthioadenosine derivatives.

[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]

[4]. 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]

[5]. 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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

CGS 21680

14 Cited Publications

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CGS 21680

GPCR/G Protein Compound Library

Small Molecule Immuno-Oncology Compound Library

Neurotransmitter Receptor Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Activators Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

RNA Binding Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) CGS 21680

Alle Adenosine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (14)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CGS 21680

GPCR/G Protein Compound Library

Small Molecule Immuno-Oncology Compound Library

Neurotransmitter Receptor Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Activators Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

RNA Binding Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) CGS 21680

Alle Adenosine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (14)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CGS 21680 Related Classifications

HY-13201 Related Classifications