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Biological Activity for BAY 60-6583
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.
Compound Libraries for BAY 60-6583
Technical Data for BAY 60-6583
|Storage||Store at +4°C|
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 Data for BAY 60-6583
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for BAY 60-6583
The following data is based on the product molecular weight 379.44. 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.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.64 mL||13.18 mL||26.35 mL|
|5 mM||0.53 mL||2.64 mL||5.27 mL|
|10 mM||0.26 mL||1.32 mL||2.64 mL|
|50 mM||0.05 mL||0.26 mL||0.53 mL|
References for BAY 60-6583
References are publications that support the biological activity of the product.
Eckle et al (2007) Cardioprotection by ecto-5'-nucleotidase (CD73) and A2B adenosine receptors. Circulation 115 1581 PMID: 17353435
van der Hoeven et al (2011) A role for the low-affinity A2B adenosine receptor in regulating superoxide generation by murine neutrophils. J.Pharmacol.Exp.Ther. 338 1004 PMID: 21693629
Auchampach et al (2009) Characterization of the A2B adenosine receptor from mouse, rabbit, and dog. J.Pharmacol.Exp.Ther. 329 2 PMID: 19141710
Gao et al (2014) Probing biased/partial agonism at the G protein-coupled A2B adenosine receptor. Biochem. Pharmacol. 90 297 PMID: 24853985
Hinz et al (2014) BAY60-6583 acts as a partial agonist at adenosine A2B receptors. J.Pharmacol.Exp.Ther. 349 427 PMID: 24633424
If you know of a relevant reference for BAY 60-6583, please let us know.
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Keywords: BAY 60-6583, BAY 60-6583 supplier, BAY60-6583, adenosine, A2B, receptor, partial, agonists, agonism, potent, cAMP, cardioprotective, ischemia, superoxide, neutrophils, ERK1/2, biased, Adenosine, Receptors, 4472, Tocris Bioscience
11 Citations for BAY 60-6583
Citations are publications that use Tocris products. Selected citations for BAY 60-6583 include:
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
Asano (2017) Aminophylline suppresses stress-induced visceral hypersensitivity and defecation in irritable bowel syndrome. Scientific Reports 7 40214 PMID: 28054654
Song (2017) Erythrocytes retain hypoxic adenosine response for faster acclimatization upon re-ascent. Nat Commun 8 14108 PMID: 28169986
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
Shih et al (2019) Dysregulation of ectonucleotidase-mediated extracellular adenosine during postmenopausal bone loss. Sci Adv 5 eaax1387 PMID: 31457100
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
Aherne et al (2015) Epithelial-specific A2B adenosine receptor signaling protects the colonic epithelial barrier during acute colitis. Autophagy 8 1324 PMID: 25850656
Mertens et al (2018) Switching-Off Adora2b in Vascular Smooth Muscle Cells Halts the Development of Pulmonary Hypertension. Front Physiol 9 555 PMID: 29910735
Iannone et al (2013) Blockade of A2b adenosine receptor reduces tumor growth and immune suppression mediated by myeloid-derived suppressor cells in a mouse model of melanoma. Neoplasia 15 1400 PMID: 24403862
Wilson et al (2016) Differences in the Phosphorylation-Dependent Regulation of Prenylation of Rap1A and Rap1B. J Mol Biol 428 4929 PMID: 27760305
Merighi (2016) A2B adenosine receptors stimulate IL-6 production in primary murine microglia through p38 MAPKkinase pathway. Pharmacological Res 117 9 PMID: 27974241
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Literature in this Area
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