BAY 60-6583 |
Catalog No.GC18114 |
Potent A2B receptor agonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 910487-58-0
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
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. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
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