Chemical Name: 2-[[6-Amino-3,5-dicyano-4-[4-(cyclopropylmethoxy)phenyl]-2-pyridinyl]thio]-acetamide
Biological ActivityBAY 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Cardioprotection by ecto-5'-nucleotidase (CD73) and A2B adenosine receptors.
Eckle et al.
A role for the low-affinity A2B adenosine receptor in regulating superoxide generation by murine neutrophils.
van der Hoeven et al.
Characterization of the A2B adenosine receptor from mouse, rabbit, and dog.
Auchampach et al.
Probing biased/partial agonism at the G protein-coupled A2B adenosine receptor.
Gao et al.
Biochem. Pharmacol., 2014;90:297
Citations for BAY 60-6583
The citations listed below are publications that use Tocris products. Selected citations for BAY 60-6583 include:
11 Citations: Showing 1 - 10
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
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.
Nat Commun 2017;8:14108
Aminophylline suppresses stress-induced visceral hypersensitivity and defecation in irritable bowel syndrome.
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.
Pharmacological Res 2016;117:9
Epithelial-specific A2B adenosine receptor signaling protects the colonic epithelial barrier during acute colitis.
Authors: Aherne Et al.
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.
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