BAY 60-6583

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4472/10
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%

Product Details
Citations (19)
Supplemental Products
Reviews

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

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

  1. 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.
  2. 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.
  3. Cardioprotection by ecto-5'-nucleotidase (CD73) and A2B adenosine receptors.
    Eckle et al.
    Circulation, 2007;115:1581
  4. 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
  5. Characterization of the A2B adenosine receptor from mouse, rabbit, and dog.
    Auchampach et al.
    J.Pharmacol.Exp.Ther., 2009;329:2
  6. Probing biased/partial agonism at the G protein-coupled A2B adenosine receptor.
    Gao et al.
    Biochem. Pharmacol., 2014;90:297
  7. 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):.

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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

  1. 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
  2. Regionally selective cardiovascular responses to adenosine A2A and A2B receptor activation.
    Authors: Mark Et al.
    FASEB J  2022;36:e22214
  3. Antitumoral Action of Resveratrol Through Adenosinergic Signaling in C6 Glioma Cells.
    Authors: Mairena Et al.
    Front Neurosci  2021;15:702817
  4. 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
  5. CD73+ extracellular vesicles inhibit angiogenesis through adenosine A2B receptor signalling.
    Authors: Stephanie Et al.
    J Extracell Vesicles  2020;9:1757900
  6. Adenosine/A2B Receptor Signaling Ameliorates the Effects of Aging and Counteracts Obesity.
    Authors: Gemma Et al.
    Cell Metab  2020;32:56-70.e7
  7. 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
  8. Dysregulation of ectonucleotidase-mediated extracellular adenosine during postmenopausal bone loss.
    Authors: Shih Et al.
    Sci Adv  2019;5:eaax1387
  9. Adenosine Attenuates Aortic Smooth Muscle Cell Calcification through A3 Adenosine Receptor.
    Authors: Tomoaki Et al.
    Tohoku J Exp Med  2019;249:275-283
  10. 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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