910487-58-0

Usage

Uses

Used in Cardiovascular Applications:
BAY 60-6583 is used as a cardioprotective agent for its protective effects against ischemia in the heart. This makes it a promising candidate for the treatment of conditions associated with reduced blood flow to the heart muscle.
Used in Renal Applications:
In the field of nephrology, BAY 60-6583 is used as a renoprotective agent, exhibiting protective effects against ischemia in the kidneys. This suggests its potential use in treating kidney diseases and conditions that involve reduced blood flow to the renal tissues.
Used in Pulmonary Applications:
BAY 60-6583 is used as a therapeutic drug for the treatment of acute lung injury. Its role in modulating adenosine A2B receptors may contribute to its protective effects in lung tissues, offering a new approach to managing lung injuries and related conditions.

Biological Activity

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.

Upstream product

• 123-08-0 4-hydroxy-benzaldehyde 
• 164521-00-0 4-(cyclobutylmethoxy)benzaldehyde 
• 910487-63-7 4-methylmorpholin-4-ium 6-amino-3,5-dicyano-4-[4-(cyclopropylmethoxy)phenyl]pyridine-2-thiolate 
• 683-57-8 bromo-acetic acid amide 

Relevant academic research and scientific papers

The aminopyridine-3,5-dicarbonitrile core for the design of new non-nucleoside-like agonists of the human adenosine A2B receptor

A new series of amino-3,5-dicyanopyridines (3–28) as analogues of the adenosine hA2B receptor agonist BAY60-6583 (compound 1) was synthesized. All the compounds that interact with the hA2B adenosine receptor display EC50 v

USE OF SUBSTITUTED 2-THIO-3,5-DICYANO-4-PHENYL-6-AMINOPYRIDINES FOR THE TREATMENT OF REPERFUSION INJURY AND REPERFUSION DAMAGE

The invention relates to substituted 2-thio-3,5-dicyano-4-phenyl-6-aminopyridines of formula (I) and their use in medicaments for the prophylaxis and/or treatment of reperfusion injury and damage.