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BAY 60-6583

Catalog No. T14506   CAS 910487-58-0

BAY 60-6583 is a potent, high-affinity adenosine A2B receptor agonist (EC50 = 3 nM) with affinity for A2B receptors that exceeds that for A1, A2A, and A3 receptors.BAY 60-6583 is cardioprotective in a model of myocardial ischemia.The Ki values for BAY 60-6583 binding to mouse, rabbit, and dog A2BAR were 750 nM, 340 nM, and 330 nM, respectively. The Ki values of BAY 60-6583 binding to A2BAR in mice, rabbits and dogs were 750 nM, 340 nM and 330 nM respectively.

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BAY 60-6583 Chemical Structure
BAY 60-6583, CAS 910487-58-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 41.00
5 mg In stock $ 98.00
10 mg In stock $ 125.00
25 mg In stock $ 258.00
50 mg In stock $ 490.00
100 mg In stock $ 742.00
500 mg In stock $ 1,550.00
1 mL * 10 mM (in DMSO) In stock $ 108.00
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Purity: 99.10%
Purity: 98.87%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description BAY 60-6583 is a potent, high-affinity adenosine A2B receptor agonist (EC50 = 3 nM) with affinity for A2B receptors that exceeds that for A1, A2A, and A3 receptors.BAY 60-6583 is cardioprotective in a model of myocardial ischemia.The Ki values for BAY 60-6583 binding to mouse, rabbit, and dog A2BAR were 750 nM, 340 nM, and 330 nM, respectively. The Ki values of BAY 60-6583 binding to A2BAR in mice, rabbits and dogs were 750 nM, 340 nM and 330 nM respectively.
Targets&IC50 A2BAR (mouse):750 nM, A2BAR (rabbit):340 nM, A2B:3 nM(EC50), A2BAR (dog):330 nM
In vitro BAY 60-6583(0-10 μM) exhibits the maximum agonist effect of BAY 60-6583 in the absence of siRNA is 68 %.[3]
BAY 60-6583 (5 μM; 24 h) induces a rise in cell accumulation within the G1 phase while concurrently reducing the G2/M phase in RAW264.7 preosteoclasts. Additionally, under the same conditions, BAY 60-6583 specifically impedes Akt activation triggered by M-CSF, with no discernible impact on M-CSF-induced ERK1/2 activation in RAW264.7 preosteoclasts.[4]
In vivo BAY 60-6583 (100 mg/kg; intravenous injection; rabbit) administered just before reperfusion, diminishes the infarction area in ischemic rabbit hearts.[1]
BAY 60-6583 (2 mg/kg; intravenous injection; mice) attenuates LPS-induced lung injury, pre-treatment with this compound can significantly decrease LPS-increased, IL-6 levels in WT mice.[2]
Molecular Weight 379.44
Formula C19H17N5O2S
CAS No. 910487-58-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 90.0 mg/mL (237.2 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Aherne CM, et al. Epithelial-specific A2B adenosine receptor signaling protects the colonic epithelial barrier during acute colitis.Mucosal Immunol. 2015 Nov;8(6):1324-38. 2. Schingnitz U, et al. Signaling through the A2B adenosine receptor dampens endotoxin-induced acute lung injury.J Immunol. 2010 May 1;184(9):5271-9. 3. Gao ZG, et al. Probing biased/partial agonism at the G protein-coupled A(2B) adenosine receptor.Biochem Pharmacol. 2014 Aug 1;90(3):297-306. 4. Yoon Taek Oh, et al. A2B Adenosine Receptor Stimulation Down-regulates M-CSF-mediated Osteoclast Proliferation. Biomed Sci Letters 2017;23:194-200 5. John A. Auchampach, et al. Characterization of the A2B Adenosine Receptor from Mouse, Rabbit, and Dog. J Pharmacol Exp Ther. 2009 Apr;329(1):2-13.  6. Morello S1, et al. Targeting the adenosine A2b receptor in the tumor microenvironment overcomes local immunosuppression by myeloid-derived suppressor cells.Oncoimmunology. 2014 Feb 14;3:e27989. eCollection 2014.

Related compound libraries

This product is contained In the following compound libraries:
GPCR Compound Library Membrane Protein-targeted Compound Library Neuronal Signaling Compound Library Bioactive Compound Library Bioactive Compounds Library Max

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Keywords

BAY 60-6583 910487-58-0 GPCR/G Protein Neuroscience Others Adenosine Receptor BAY 606583 BAY 60 6583 inhibitor inhibit

 

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