BAY 60-6583

Catalog #: 4472
19 Citations Datasheet / COA / SDS

Catalog #	Availability	Size / Price	Qty
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4472/50

BAY 60-6583 | CAS No. 910487-58-0 | Adenosine A2b Receptor Agonists

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Description: Potent partial A2B agonist; cardioprotective

Chemical Name: 2-[[6-Amino-3,5-dicyano-4-[4-(cyclopropylmethoxy)phenyl]-2-pyridinyl]thio]-acetamide

Purity: ≥98%

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Product Details

Citations (19)

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Biological Activity

BAY 60-6583 is a partial agonist at adenosine A_2B receptors (EC₅₀ = 2.83 nM for murine A_2B receptor). Displays selectivity for A_2B over A₁, A_2Aand 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

M.Wt:

379.44

Formula:

C₁₉H₁₇N₅O₂S

Solubility:

Soluble to 100 mM in DMSO

Purity:

≥98%

Storage:

Store at +4°C

CAS No:

910487-58-0

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

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 A_2B 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 A_2B adenosine receptor.
Gao et al.
Biochem. Pharmacol., 2014;90:297

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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

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
Regionally selective cardiovascular responses to adenosine A2A and A2B receptor activation.
Authors: Mark Et al.
FASEB J 2022;36:e22214
Antitumoral Action of Resveratrol Through Adenosinergic Signaling in C6 Glioma Cells.
Authors: Mairena Et al.
Front Neurosci 2021;15:702817
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
CD73+ extracellular vesicles inhibit angiogenesis through adenosine A2B receptor signalling.
Authors: Stephanie Et al.
J Extracell Vesicles 2020;9:1757900
Adenosine/A2B Receptor Signaling Ameliorates the Effects of Aging and Counteracts Obesity.
Authors: Gemma Et al.
Cell Metab 2020;32:56-70.e7
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
Dysregulation of ectonucleotidase-mediated extracellular adenosine during postmenopausal bone loss.
Authors: Shih Et al.
Sci Adv 2019;5:eaax1387
Adenosine Attenuates Aortic Smooth Muscle Cell Calcification through A3 Adenosine Receptor.
Authors: Tomoaki Et al.
Tohoku J Exp Med 2019;249:275-283
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

Switching-Off Adora2b in Vascular Smooth Muscle Cells Halts the Development of Pulmonary Hypertension.
Authors: Mertens Et al.
Front Physiol 2018;9:555

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

Erythrocytes retain hypoxic adenosine response for faster acclimatization upon re-ascent.
Authors: Song
Nat Commun 2017;8:14108

Aminophylline suppresses stress-induced visceral hypersensitivity and defecation in irritable bowel syndrome.
Authors: Asano
Scientific Reports 2017;7:40214

Differences in the Phosphorylation-Dependent Regulation of Prenylation of Rap1A and Rap1B.
Authors: Wilson Et al.
J Mol Biol 2016;428:4929

A2B adenosine receptors stimulate IL-6 production in primary murine microglia through p38 MAPKkinase pathway.
Authors: Merighi
Pharmacological Res 2016;117:9

Epithelial-specific A2B adenosine receptor signaling protects the colonic epithelial barrier during acute colitis.
Authors: Aherne Et al.
Autophagy 2015;8:1324

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

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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