BAY 60-6583
Chemical Name: 2-[[6-Amino-3,5-dicyano-4-[4-(cyclopropylmethoxy)phenyl]-2-pyridinyl]thio]-acetamide
Purity: ≥98%
Biological Activity
BAY 60-6583 is a partial agonist at adenosine A2B receptors (EC50 = 2.83 nM for murine A2B receptor). Displays selectivity for A2B over A1, A2A and A3 receptors. BAY 60-6583 antagonizes the effect of NECA (Cat. No. 1691) and adenosine (Cat. No. 3624) in cAMP accumulation assays. Decreases fMLP-induced superoxide production in neutrophils at low concentrations (1-10 nM). Cardioprotective; attenuates infarct size in a mouse model of myocardial ischemia. Exhibits ERK1/2-biased agonism.Technical Data
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.
Background References
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IFN-gamma Prevents Adenosine Receptor (A2bR) Upregulation To Sustain the Macrophage Activation Response.
Cohen H, Ward A, Hamidzadeh K, Ravid K, Mosser D
J Immunol, 2015;195(8):3828-37. -
Intestinal immunopathology is associated with decreased CD73-generated adenosine during lethal infection.
Francois V, Shehade H, Acolty V, Preyat N, Delree P, Moser M, Oldenhove G
Mucosal Immunol, 2015;8(4):773-84. -
Cardioprotection by ecto-5'-nucleotidase (CD73) and A2B adenosine receptors.
Eckle et al.
Circulation, 2007;115:1581 -
A role for the low-affinity A2B adenosine receptor in regulating superoxide generation by murine neutrophils.
van der Hoeven et al.
J.Pharmacol.Exp.Ther., 2011;338:1004 -
Characterization of the A2B adenosine receptor from mouse, rabbit, and dog.
Auchampach et al.
J.Pharmacol.Exp.Ther., 2009;329:2 -
Probing biased/partial agonism at the G protein-coupled A2B adenosine receptor.
Gao et al.
Biochem. Pharmacol., 2014;90:297 -
Stimulation of the adenosine A3 receptor, not the A1 or A2 receptors, promote neurite outgrowth of retinal ganglion cells
KI Nakashima, K Iwao, T Inoue, A Haga, T Tsutsumi, MI Mochita, T Fujimoto, H Tanihara
Exp. Eye Res., 2018;0(0):.
Product Datasheets
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Citations for BAY 60-6583
The citations listed below are publications that use Tocris products. Selected citations for BAY 60-6583 include:
19 Citations: Showing 1 - 10
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Adenosine metabolized from extracellular ATP promotes type 2 immunity through triggering A2BAR signaling in intestinal epithelial cells.
Authors: Fei Et al.
Cell Rep 2022;40:111150
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Regionally selective cardiovascular responses to adenosine A2A and A2B receptor activation.
Authors: Mark Et al.
FASEB J 2022;36:e22214
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Antitumoral Action of Resveratrol Through Adenosinergic Signaling in C6 Glioma Cells.
Authors: Mairena Et al.
Front Neurosci 2021;15:702817
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Pharmacological Insights Into Safety and Efficacy Determinants for the Development of Adenosine Receptor Biased Agonists in the Treatment of Heart Failure.
Authors: Stefano Et al.
Front Pharmacol 2021;12:628060
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CD73+ extracellular vesicles inhibit angiogenesis through adenosine A2B receptor signalling.
Authors: Stephanie Et al.
J Extracell Vesicles 2020;9:1757900
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Adenosine/A2B Receptor Signaling Ameliorates the Effects of Aging and Counteracts Obesity.
Authors: Gemma Et al.
Cell Metab 2020;32:56-70.e7
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Adenosine A2A receptor stimulation restores cell functions and differentiation in Niemann-Pick type C-like oligodendrocytes.
Authors: Nuccio Et al.
Sci Rep 2019;9:9782
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Dysregulation of ectonucleotidase-mediated extracellular adenosine during postmenopausal bone loss.
Authors: Shih Et al.
Sci Adv 2019;5:eaax1387
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Adenosine Attenuates Aortic Smooth Muscle Cell Calcification through A3 Adenosine Receptor.
Authors: Tomoaki Et al.
Tohoku J Exp Med 2019;249:275-283
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Adenosine Receptor Signaling Targets Both PKA and Epac Pathways to Polarize Dendritic Cells to a Suppressive Phenotype.
Authors: Caglar Et al.
J Immunol 2019;203:3247-3255
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Switching-Off Adora2b in Vascular Smooth Muscle Cells Halts the Development of Pulmonary Hypertension.
Authors: Mertens Et al.
Front Physiol 2018;9:555
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Melanotan II causes hypothermia in mice by activation of mast cells and stimulation of histamine 1 receptors.
Authors: Jain Et al.
Am J Physiol Endocrinol Metab 2018;315:E357
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Erythrocytes retain hypoxic adenosine response for faster acclimatization upon re-ascent.
Authors: Song
Nat Commun 2017;8:14108
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Aminophylline suppresses stress-induced visceral hypersensitivity and defecation in irritable bowel syndrome.
Authors: Asano
Scientific Reports 2017;7:40214
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Differences in the Phosphorylation-Dependent Regulation of Prenylation of Rap1A and Rap1B.
Authors: Wilson Et al.
J Mol Biol 2016;428:4929
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A2B adenosine receptors stimulate IL-6 production in primary murine microglia through p38 MAPKkinase pathway.
Authors: Merighi
Pharmacological Res 2016;117:9
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Epithelial-specific A2B adenosine receptor signaling protects the colonic epithelial barrier during acute colitis.
Authors: Aherne Et al.
Autophagy 2015;8:1324
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Apremilast, a novel phosphodiesterase 4 (PDE4) inhibitor, regulates inflammation through multiple cAMP downstream effectors.
Authors: Perez-Aso Et al.
Arthritis Res Ther 2015;17:249
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Blockade of A2b adenosine receptor reduces tumor growth and immune suppression mediated by myeloid-derived suppressor cells in a mouse model of melanoma.
Authors: Iannone Et al.
Neoplasia 2013;15:1400
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