CGS 21680 hydrochloride

Name: CGS 21680 hydrochloride
Brand: Tocris Bioscience
SKU: 1063
Rating: 5 (3 reviews)

Catalog # 1063

Citations (73)

(3)

COA / SDS

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Key Product Details

Description:	A_2A agonist
Chemical Name:	4-[2-[[6-Amino-9-(N-ethyl-β-D-ribofuranuronamidosyl)-9H-purin-2-yl]amino]ethyl]benzenepropanoic acid hydrochloride
Purity:	≥98% (HPLC)
Molecular Weight:	535.99

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Biological Activity

CGS 21680 hydrochloride is a potent A_2A adenosine receptor agonist (K_i = 27 nM, EC₅₀ = 1.48-180 nM). CGS 21680 reduces venous resistance, increases heart rate and cardiac output in vivo. In an animal model of Huntington's disease, CGS21680 slows motor deterioration, prevents reduction in brain weight and reduces the size of mutant huntingtin aggregates and intranuclear inclusions. CGS21680 increases proliferation of neural progenitor cells, promotes survival of motoneurons and activates TrkB receptors. Also has anti-inflammatory effects in animal models of lung injury and reduces neurotoxicity induced by Kainate (Cat. No. 7065).

Compound Libraries

CGS 21680 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	535.99
Formula	C₂₃H₂₉N₇O₆.HCl
Storage	Desiccate at -20°C
Purity	≥98% (HPLC)
CAS Number	124431-80-7
PubChem ID	10256643
InChi Key	QPHVMNOEKKJYJO-MJWSIIAUSA-N
Smiles	NC1=NC(NCCC4=CC=C(CCC(O)=O)C=C4)=NC2=C1N=CN2[C@@H]3O[C@H]([C@](NCC)=O)[C@@H](O)[C@H]3O.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	53.6	100

Preparing Stock Solutions

The following data is based on the product molecular weight 535.99.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.87 mL	9.33 mL	18.66 mL
5 mM	0.37 mL	1.87 mL	3.73 mL
10 mM	0.19 mL	0.93 mL	1.87 mL
50 mM	0.04 mL	0.19 mL	0.37 mL

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References

References are publications that support the biological activity of the product.

Komaki Trk and cAMP-dependent survival activity of adenosine A(2A) agonist CGS21680 on rat motoneurons in culture. Neurosci.Lett. 2012 PMID: 22691937
Wiese Adenosine receptor A_2A-R contributes to motoneuron survival by transactivating the tyrosine kinase receptor TrkB Proc.Natl.Acad.Sci.U.S.A. 2007 PMID: 17940030
Chou CGS21680 attenuates symptoms of Huntington's disease in a transgenic mouse model. J.Neurochem. 2005 PMID: 15816854
Rebola Different roles of adenosine A₁, A_2A and A₃ receptors in controlling kainate-induced toxicity in cortical cultured neurons. Neurochem.Int. 2005 PMID: 16011860
Klot Adenosine receptors and their ligands. Naunyn Schmiedebergs Arch.Pharmacol. 2000 PMID: 11111832
Nekooeian and Tabrizchi Effects of CGS 21680, a selective A_2A adenosine receptor agonist, on cardiac output and vascular resistance in acute heart failure in the anaesthetized rat. Br.J.Pharmacol. 1998 PMID: 9605574
Shryock A_2A-adenosine receptor reserve for coronary vasodilation. Circulation 1998 PMID: 9715864
Phillis The selective adenosine A₂ receptor agonist, CGS 21680, is a potent depressant of cerebral cortical neuronal activity. Brain Res. 1990 PMID: 2322828

Citations for CGS 21680 hydrochloride (73)

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Citations are publications that use Bio-Techne products. Selected citations for CGS 21680 hydrochloride include:

Kong et al. (2019) Adenosine A2a receptor agonist CGS21680 treatment attenuates cardiopulmonary bypass-associated inflammatory lung injury in juvenile rats. Mol.Med.Rep.. 20:117
PMID: 31115565
Nuccio et al. (2019) Adenosine A2A receptor stimulation restores cell functions and differentiation in Niemann-Pick type C-like oligodendrocytes. Sci Rep. 9:9782
PMID: 31278313
Jain et al. (2018) Melanotan II causes hypothermia in mice by activation of mast cells and stimulation of histamine 1 receptors. Am J Physiol Endocrinol Metab. 315:E357
PMID: 29812984
Shifrut et al. (2018) Genome-wide CRISPR Screens in Primary Human T Cells Reveal Key Regulators of Immune Function. Cell. 175:1958
PMID: 30449619
Núñez et al. (2018) PBF509, an Adenosine A2A Receptor Antagonist With Efficacy in Rodent Models of Movement Disorders. Front Pharmacol. 9:1200
PMID: 30405415
Bakhshayesh et al. (2017) The Mediating Role of A2A Adenosine Receptors in the Mitochondrial Pathway of Apoptotic Hippocampal Cell Death, Following the Administration of MDMA in Rat. Basic Clin Neurosci. 8:317
PMID: 29158882
Ledderose et al. (2016) Adenosine arrests breast cancer cell motility by A3 receptor stimulation. Purinergic Signalling. 2016;
PMID: 27577957
Liu et al. (2016) Activation of Adenosine 2A receptor inhibits neutrophil apoptosis in an autophagy-dependent manner in mice with systemic inflammatory response syndrome. Scientific Reports. 6:33614
PMID: 27647162
Caiazzo et al. (2016) Adenosine signalling mediates the anti-inflammatory effects of the COX-2 inhibitor nimesulide. Biochem.Pharmacol.. 112:72
PMID: 27188793
Ferreira et al. (2015) Presynaptic adenosine A2A receptors dampen cannabinoid CB1 receptor-mediated inhibition of corticostriatal glutamatergic transmission. Br J Pharmacol. 172:1074
PMID: 25296982
Kavanagh et al. (2015) Role of adenosine receptor subtypes in metha. reward and reinforcement. J Neurogenet. 89:265
PMID: 25301277
Eusemann et al. (2015) Adenosine Receptors Differentially Regulate the Expression of Regulators of G-Protein Signalling (RGS) 2, 3 and 4 in Astrocyte-Like Cells. PLoS One. 10:e0134934
PMID: 26263491
Perez-Aso et al. (2015) Apremilast, a novel phosphodiesterase 4 (PDE4) inhibitor, regulates inflammation through multiple cAMP downstream effectors. Arthritis Res Ther. 17:249
PMID: 26370839
Kermanian et al. (2015) Effects of adenosine A2a receptor agonist and antagonist on cerebellar nuclear factor-kB expression preceded by MDMA toxicity. Eneuro. 28:120
PMID: 25678999
Polito et al. (2015) Selective Effects of PDE10A Inhibitors on Striatopallidal Neurons Require Phosphatase Inhibition by DARPP-32(1,2,3). Mol Cell Biol. 2
PMID: 26465004
Tosolini et al. (2015) Human monocyte recognition of adenosine-based cyclic dinucleotides unveils the A2a Gαs protein-coupled receptor tonic inhibition of mitochondrially induced cell death. Psychopharmacology (Berl). 35:479
PMID: 25384972
Wydra et al. (2015) On the role of A2A and D2 receptors in control of cocaine and food-seeking behaviors in rats. Am J Respir Cell Mol Biol. 232:1767
PMID: 25420611
Welihinda and Amento (2014) Positive allosteric modulation of the adenosine A2a receptor attenuates inflammation. J Inflamm (Lond). 11:37
PMID: 25473378
O'Neill et al. (2014) Persistent reduction of cocaine seeking by pharmacological manipulation of adenosine A1 and A 2A receptors during extinction training in rats. Psychopharmacology (Berl). 231:3179
PMID: 24562064
Perígolo-Vicente et al. (2014) IL-6, A1 and A2aR: a crosstalk that modulates BDNF and induces neuroprotection. Biochem Biophys Res Commun. 449:477
PMID: 24845382
Chen et al. (2014) Prolonged adenosine A1 receptor activation in hypoxia and pial vessel disruption focal cortical ischemia facilitates clathrin-mediated AMPA receptor endocytosis and long-lasting synaptic inhibition in rat hippocampal CA3-CA1 synapses: differential regulat J Neurosci. 34:9621
PMID: 25031403
Ahsan and Mehal (2014) Activation of adenosine receptor A2A increases HSC proliferation and inhibits death and senescence by down-regulation of p53 and Rb. Front Pharmacol. 5:69
PMID: 24782773
Ruby et al. (2014) Adenosinergic regulation of striatal clock gene expression and ethanol intake during constant light. Kidney Int. 39:2432
PMID: 24755889
Ziemlinska et al. (2014) Overexpression of BDNF increases excitability of the lumbar spinal network and leads to robust early locomotor recovery in completely spinalized rats. PLoS One. 9:e88833
PMID: 24551172
Li et al. (2014) Regulation of photoreceptor gap junction phosphorylation by adenosine in zebrafish retina. Vis Neurosci. 31:237
PMID: 24844306
Kozma et al. (2013) Characterization by flow cytometry of fluorescent, selective agonist probes of the A(3) adenosine receptor. Biochem Pharmacol. 85:1171
PMID: 23376019
Yang et al. (2013) Adenosine A2A receptor contributes to ischemic brain damage in newborn piglet. J Cereb Blood Flow Metab. 33:1612
PMID: 23860373
Garção et al. (2013) Functional interaction between pre-synaptic α6β2-containing nicotinic and adenosine A2A receptors in the control of DA release in the rat striatum. Br J Pharmacol. 169:1600
PMID: 23638679
Fernández-Dueñas et al. (2013) DA D(2) receptor-mediated modulation of adenosine A(2A) receptor agonist binding within the A(2A)R/D(2)R oligomer framework. FASEB J. 63:42
PMID: 23619397
Loram et al. (2013) Intrathecal injection of adenosine 2A receptor agonists reversed neuropathic allodynia through protein kinase (PK)A/PKC signaling. Brain Behav Immun. 33:112
PMID: 23811314
Bao et al. (2013) Pannexin 1 channels link chemoattractant receptor signaling to local excitation and global inhibition responses at the front and back of polarized neutrophils. J Biol Chem. 288:22650
PMID: 23798685
Aggarwal et al. (2013) Macrophage A2A adenosinergic receptor modulates oxygen-induced augmentation of murine lung injury. Neuropsychopharmacology. 48:635
PMID: 23349051
Thomas et al. (2013) Design and evaluation of xanthine based adenosine receptor antagonists: potential hypoxia targeted immunotherapies. Bioorg Med Chem. 21:7453
PMID: 24126093
Lee (2013) Both MC5r and A2Ar are required for protective regulatory immunity in the spleen of post-experimental autoimmune uveitis in mice. J Immunol. 191:4103
PMID: 24043903
Wiseman et al. (2013) Proteasomal degradation of eukaryotic elongation factor-2 kinase (EF2K) is regulated by cAMP-PKA signaling and the SCFβTRCP ubiquitin E3 ligase. J Biol Chem. 288:17803
PMID: 23640883
Matos et al. (2013) Antagonistic interaction between adenosine A2A receptors and Na+/K+-ATPase-α2 controlling glutamate uptake in astrocytes. J Neurosci. 33:18492
PMID: 24259572
He et al. (2013) Adenosine regulates bone metabolism via A1, A2A, and A2B receptors in bone marrow cells from normal humans and patients with multiple myeloma. FASEB J. 27:3446
PMID: 23682121
Xiao et al. (2013) Adenosine A2A receptor: a target for regulating renal interstitial fibrosis in obstructive nephropathy. PLoS One. 8:e60173
PMID: 23585831
Kan et al. (2012) Imiquimod suppresses propagation of herpes simplex virus 1 by upregulation of cystatin A via the adenosine receptor A1 pathway. J Virol. 86:10338
PMID: 22787201
Jeon et al. (2012) Oroxylin A Induces BDNF Expression on Cortical Neurons through Adenosine A2A Receptor Stimulation: A Possible Role in Neuroprotection. Neurochem Int. 20:27
PMID: 24116271
Park et al. (2012) Proximal tubule sphingosine kinase-1 has a critical role in A1 adenosine receptor-mediated renal protection from ischemia. Kidney Int. 82:878
PMID: 22695326
Fernández-Dueñas et al. (2012) Molecular determinants of A2AR-D2R allosterism: role of the intracellular loop 3 of the D2R. J Immunol. 123:373
PMID: 22924752
Mills et al. (2012) Extracellular adenosine signaling induces CX3CL1 expression in the brain to promote experimental autoimmune encephalomyelitis. J Neurochem. 9:193
PMID: 22883932
O'Neill et al. (2012) Adenosine A2A receptors in the nucleus accumbens bi-directionally alter cocaine seeking in rats. Neuropsychopharmacology. 37:1245
PMID: 22169945
Lee et al. (2012) When cytokinin, a plant hormone, meets the adenosine A2A receptor: a novel neuroprotectant and lead for treating neurodegenerative disorders? PLoS One. 7:e38865
PMID: 22719969
Mediero et al. (2012) Adenosine A2A receptor activation prevents wear particle-induced osteolysis. Sci Transl Med. 4:135ra65
PMID: 22623741
Hobson et al. (2012) Stimulation of adenosine receptors in the nucleus accumbens reverses the expression of cocaine sensitization and cross-sensitization to DA D2 receptors in rats. Neuropharmacology. 63:1172
PMID: 22749927
Kiebala and Maggirwar (2011) Ibudilast, a pharmacologic phosphodiesterase inhibitor, prevents human immunodeficiency virus-1 Tat-mediated activation of microglial cells. PLoS One. 6:e18633
PMID: 21494611
Carlström et al. (2011) Adenosine A2A receptor activation attenuates tubuloglomerular feedback responses by stimulation of endothelial nitric oxide synthase. Am J Physiol Renal Physiol. 300:F457
PMID: 21106859
Su et al. (2011) Receptor desensitization and blockade of the suppressive effects of prostaglandin E(2) and adenosine on the cytotoxic activity of human melanoma-infiltrating T lymphocytes. Cancer Immunol Immunother. 60:111
PMID: 20960188
Ru et al. (2011) Adenosine-induced activation of esophageal nociceptors. Am J Physiol Gastrointest Liver Physiol. 300:G485
PMID: 21148396
Garcia et al. (2011) Adenosine A(2A) receptor activation prevents progressive kidney fibrosis in a model of immune-associated chronic inflammation. PLoS One. 80:378
PMID: 21508927
Zhou et al. (2010) GSK-3alpha directly regulates beta-adrenergic signaling and the response of the heart to hemodynamic stress in mice. J Clin Invest. 120:2280
PMID: 20516643
Garavaglia et al. (2010) Adaptation of NS cells growth and differentiation to high-throughput screening-compatible plates. BMC Neurosci. 11:7
PMID: 20085655
Hiranita et al. (2010) Reinforcing effects of sigma-receptor agonists in rats trained to self-administer cocaine. J Pharmacol Exp Ther. 332:515
PMID: 19892920
Gebremedhin et al. (2010) Adenosine can mediate its actions through generation of reactive oxygen species. J Cereb Blood Flow Metab. 30:1777
PMID: 20531463
Wang et al. (2010) Static magnetic field exposure reproduces cellular effects of the Parkinson's disease drug candidate ZM241385. Biomol Ther (Seoul). 5:e13883
PMID: 21079735
Das et al. (2010) Nucleoside conjugates of quantum dots for characterization of G protein-coupled receptors: strategies for immobilizing A2A adenosine receptor agonists. J Nanobiotechnology. 8:11
PMID: 20478037
Higley and Sabatini (2010) Competitive regulation of synaptic Ca²⁺ influx by D2 DA and A2A adenosine receptors. Nat Neurosci. 13:958
PMID: 20601948
Keene et al. (2010) Multivalent dendrimeric and monomeric adenosine agonists attenuate cell death in HL-1 mouse cardiomyocytes expressing the A(3) receptor. Biochem Pharmacol. 80:188
PMID: 20346920
Nowak et al. (2010) The A2aR adenosine receptor controls cytokine production in iNKT cells. Neuropharmacology. 40:682
PMID: 20039304
Xi et al. (2009) Adenosine A2A and A2B receptors work in concert to induce a strong protection against reperfusion injury in rat hearts. J Mol Cell Cardiol. 47:684
PMID: 19695259
Epperson et al. (2009) Adenosine receptors and second messenger signaling pathways in rat cardiac fibroblasts. Am J Physiol Cell Physiol. 296:C1171
PMID: 19244482
Ohta et al. (2009) A2A adenosine receptor may allow expansion of T cells lacking effector functions in extracellular adenosine-rich microenvironments. Eur J Immunol. 183:5487
PMID: 19843934
Pugliese et al. (2009) The adenosine A2A receptor antagonist ZM241385 enhances neuronal survival after oxygen-glucose deprivation in rat CA1 hippocampal slices. Br J Pharmacol. 157:818
PMID: 19422385
Shen et al. (2008) Dichotomous DArgic control of striatal synaptic plasticity. Science. 321:848
PMID: 18687967
Garcia et al. (2008) Adenosine A2A receptor activation and macrophage-mediated experimental glomerulonephritis. J Neuroinflammation. 22:445
PMID: 17898087
Keir et al. (2006) Mechanism of adenosine-induced airways obstruction in allergic guinea pigs. Br J Pharmacol. 147:720
PMID: 16432507
Yang et al. (2006) The A2B adenosine receptor protects against inflammation and excessive vascular adhesion. J Clin Invest. 116:1913
PMID: 16823489
Kornerup et al. (2005) Pharmacological characterisation of the adenosine receptor mediating increased ion transport in the mouse isolated trachea and the effect of allergen challenge. Br J Pharmacol. 144:1011
PMID: 15685200
Germack and Dickenson (2004) Characterization of ERK1/2 signalling pathways induced by adenosine receptor subtypes in newborn rat cardiomyocytes. Br J Pharmacol. 141:329
PMID: 14751870
Nieri et al. (2001) Adenosine-mediated hypotension in in vivo guinea-pig: receptors involved and role of NO. Br J Pharmacol. 134:745
PMID: 11606314
Ezeamuzie and Philips (1999) Adenosine A3 receptors on human eosinophils mediate inhibition of degranulation and superoxide anion release. Br J Pharmacol. 127:188
PMID: 10369472

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HEK cell line expressing A2A Receptor

Name: Tahmineh Safaie

Species: Human

Assay Type: In Vitro

HEK cell line expressing A2A Receptor were treated with CGS in presence or absence of ZM241385 for 30 minutes and level of cAMP was measured.
works on inhibited CD4 cells

Name: Anonymous

Species: Mouse

Assay Type: In Vitro

Works perfectly on my CD4 T cells proliferation assay, when detected by CFSE. It inhibited the proliferation of activated CD4 cells in dose-dependent manner.
Cell based assays

Name: Anonymous

Species: Human

receptors, antibody or ILISA Kits

HGF protein

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