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BAY 60-6583 (BAY606583) is a novel and potent agonist of adenosine A2B receptor (EC50 = 3 nM) with cardioprotective effects in a myocardial ischemia model. The adenosine A2B receptor plays an important role in anti-inflammatory response and pre/postconditioning cardioprotective.
| ln Vitro |
In CHO cells expressing recombinant human A1, A2A, or A2B ARs, BAY 60-6583 displays EC50 values for receptor activation >10,000 nM for both A1 and A2A AR and 3 nM for A2B AR subtype[1]. When baY 60-6583 (0 -10 μM) is used without siRNA, its highest agonist effect is 68%, which is notably different from when 5, 50, and 500 nM siRNA are present (54%, 48%, and 36%, respectively). In T24 cells, it displays BAY EC50 values of 98±22, 102±17, 127±31, and 93±19 nM, respectively, in the absence and presence of siRNA[3]. In RAW264.7 preosteoclasts, BAY 60-6583 (5 μM; 24 hours) boosts cell accumulation at the G1 phase while decreasing the G2/M phase[4]. While BAY 60-6583 (5 μM; 24 hours) does not influence M-CSF-induced ERK1/2 activation in RAW264, it selectively suppresses the activation of Akt by M-CSF.[4] Seven preosteoclasts.
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| ln Vivo |
In ischemic rabbit hearts, BAY 60-6583 (intravenous injection; 100 mcg/kg) decreases the infarction area soon before reperfusion[1]. ?When used as a pre-treatment, BAY 60-6583 (intraperitoneal injection; 2 mg/kg) greatly reduces the amount of lung damage caused by lipopolysaccharide (LPS). IL-6 levels in WT-mice, although the administration of BAY 60-6583 fails to abolish these inflammatory markers in?A2BAR?//? ?mice [2]. ?Intratumoral treatment of BAY 60-6583 results in a considerable increase in tumor-infiltrating MDSCs; it has no effect on the cells' capacity to inhibit T-cell proliferation or maturation stage, and it also promotes the creation of CCL2 and IL-10 within the tumor tissue[5].
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| Cell Assay |
Cell Cycle Analysis[4]
Cell Types: RAW264.7 preosteoclasts Tested Concentrations: 5 μM Incubation Duration: 48 hrs (hours) Experimental Results: Caused an arrest of cells at the G1 phase. Western Blot Analysis[4] Cell Types: RAW264.7 preosteoclasts Tested Concentrations: 5 μM Incubation Duration: 48 hrs (hours) Experimental Results: demonstrated an inhibition of M-CSF-mediated Akt activation and resulted in the decrease of osteoclast proliferation. |
| Animal Protocol |
Animal/Disease Models: A2BAR−/− mice on a C57BL/6J mice[1]
Doses: 2 mg/kg Route of Administration: intraperitoneal (ip)injection; 2 mg/kg Experimental Results: Demonstrated attenuation of lung inflammation and pulmonary edema in wild-type but not in gene-targeted mice for the A2BAR. |
| References |
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| Additional Infomation |
BAY 60-6583 is a member of the class of cyanopyridines that is 6-amino-3,5-dicyano-4-(4-hydroxyphenyl)-2-sulfanylpyridine in which the hydroxy and sulfanyl hydrogens are replaced by cyclopropylmethyl and carboxamidomethyl groups respectively. It has a role as an adenosine A2B receptor agonist, a cardioprotective agent and an anti-inflammatory agent. It is an aminopyridine, a cyanopyridine, an aryl sulfide, a monocarboxylic acid amide, an aromatic ether and a member of cyclopropanes.
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| Molecular Formula |
C19H17N5O2S
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|---|---|
| Molecular Weight |
379.43558
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| Exact Mass |
379.11
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| CAS # |
910487-58-0
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| PubChem CID |
11717831
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| Appearance |
White to light yellow solid powder
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| LogP |
4.171
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
27
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| Complexity |
629
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ZTYHZMAZUWOXNC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H17N5O2S/c20-7-14-17(12-3-5-13(6-4-12)26-9-11-1-2-11)15(8-21)19(24-18(14)23)27-10-16(22)25/h3-6,11H,1-2,9-10H2,(H2,22,25)(H2,23,24)
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| Chemical Name |
2-[6-amino-3,5-dicyano-4-[4-(cyclopropylmethoxy)phenyl]pyridin-2-yl]sulfanylacetamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~263.55 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 4.17 mg/mL (10.99 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 41.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 4.17 mg/mL (10.99 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 41.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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