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BAY 60-6583

Catalog No.GC18114

Potent A2B receptor agonist

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BAY 60-6583 Chemical Structure

Cas No.: 910487-58-0

Size Price Stock Qty
1mg
$26.00
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5mg
$99.00
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10mg
$126.00
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25mg
$296.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

BAY 60-6583 is a selective and potent agonist of adenosine A2B receptor with EC50 value of 3 nM [1].

The adenosine A2B receptor is a G-protein coupled adenosine receptor and is activated by high concentrations adenosine. The adenosine A2B receptor plays an important role in anti-inflammatory response and pre/postconditioning cardioprotective [1].

BAY 60-6583 is a potent adenosine A2B receptor agonist. In CHO cells, BAY 60-6583 showed EC50 values of >10000, >10000 and 3 nM respectively for recombinant human A1, A2A and A2B ARs [1]. In BEAS-2B human airway epithelial cells transfected with glucocorticoid response element (GRE) reporter and cAMP-response element (CRE), BAY 60-6583 increased GRE- and CRE-dependent transcription mediated by adenosine A2B receptor that was associated with cAMP formation. Also, BAY 60-6583 increased the expression of CD200, CRISPLD2 and SOCS3, which suppressed the release of proinflammatory mediator [2]. In macrophages derived from arterial injury mice, BAY 60-6583 increased the expression of A2bAR, which then inhibited the released of tumor necrosis factor ɑ (TNF-ɑ) that promoting inflammatory response [3].

In a myocardial ischaemic injury rabbit model, BAY 60-6583 (100 mcg/kg) reduced the infarction area [1].

References:
[1].  Baraldi PG, Tabrizi MA, Fruttarolo F, et al. Recent improvements in the development of A(2B) adenosine receptor agonists. Purinergic Signal, 2008, 4(4): 287-303.
[2].  Greer S, Page CW, Joshi T, et al. Concurrent agonism of adenosine A2B and glucocorticoid receptors in human airway epithelial cells cooperatively induces genes with anti-inflammatory potential: a novel approach to treat chronic obstructive pulmonary disease. J Pharmacol Exp Ther, 2013, 346(3): 473-485.
[3].  Chen H, Yang D, Carroll SH, et al. Activation of the macrophage A2b adenosine receptor regulates tumor necrosis factor-alpha levels following vascular injury. Exp Hematol, 2009, 37(5): 533-538.

Chemical Properties

Cas No. 910487-58-0 SDF
Chemical Name 2-((6-amino-3,5-dicyano-4-(4-(cyclopropylmethoxy)phenyl)pyridin-2-yl)thio)acetamide
Canonical SMILES O=C(CSC1=NC(N)=C(C#N)C(C2=CC=C(C=C2)OCC3CC3)=C1C#N)N
Formula C19H17N5O2S M.Wt 379.44
Solubility 0.3mg/mL in ethanol, 30mg/mL in DMSO, 25mg/mL in DMF Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.6355 mL 13.1773 mL 26.3546 mL
5 mM 0.5271 mL 2.6355 mL 5.2709 mL
10 mM 0.2635 mL 1.3177 mL 2.6355 mL
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3. All of the above co-solvents are available for purchase on the GlpBio website.

Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 10 reference(s) in Google Scholar.)

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