1. GPCR/G Protein
  2. Adenosine Receptor
  3. BAY 60-6583

BAY 60-6583 

Cat. No.: HY-103171 Purity: >99.0%
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BAY 60-6583 is a potent and high-affinity agonist of adenosine A2B receptor (EC50 = 3 nM) over A1, A2A, and A3 receptors. BAY 60-6583 binds to mouse, rabbit, and dog A2BAR with Ki values of 750 nM, 340 nM and 330 nM, respectively. BAY 60-6583 has a cardioprotective effect in a myocardial ischemia model.

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BAY 60-6583 Chemical Structure

BAY 60-6583 Chemical Structure

CAS No. : 910487-58-0

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Description

BAY 60-6583 is a potent and high-affinity agonist of adenosine A2B receptor (EC50 = 3 nM) over A1, A2A, and A3 receptors. BAY 60-6583 binds to mouse, rabbit, and dog A2BAR with Ki values of 750 nM, 340 nM and 330 nM, respectively. BAY 60-6583 has a cardioprotective effect in a myocardial ischemia model[1][5].

In Vitro

BAY 60-6583 exhibits EC50 values for receptor activation >10,000 nM for both A1 and A2A AR and 3 nM for A2B AR subtype in CHO cells expressing recombinant human A1, A2A or A2B ARs[1].
BAY 60-6583(0-10 µM) exhibits the maximum agonist effect of BAY in the absence of siRNA is 68 %, which is significantly different from that in the presence of 5, 50 and 500 nM siRNA (54%, 48% and 36%, respectively). It exhibits EC50  values of BAY in the absence and presence siRNA with 98±22, 102±17, 127±31 and 93±19 nM, respectively, in T24 cells[3].
BAY 60-6583 (5 μM; 24 hours) increases the accumulation of cells at the G1 phase with a decrease in G2/M phase in RAW264.7 preosteoclasts[4].
BAY 60-6583 (5 μM; 24 hours) specifically inhibits the activation of Akt by M-CSF, whereas M-CSF-induced ERK1/2 activation is not affected by BAY 60-6583 treatment in RAW264.7 preosteoclasts[4].

Cell Cycle Analysis[4]

Cell Line: RAW264.7 preosteoclasts
Concentration: 5 μM
Incubation Time: 48 hours
Result: Caused an arrest of cells at the G1 phase.

Western Blot Analysis[4]

Cell Line: RAW264.7 preosteoclasts
Concentration: 5 μM
Incubation Time: 48 hours
Result: Exhibited an inhibition of M-CSF-mediated Akt activation and resulted in the decrease of osteoclast proliferation.
In Vivo

BAY 60-6583 (intravenous injection; 100 mcg/kg) reduces the infarction area just prior to reperfusion in ischaemic rabbit hearts[1].
BAY 60-6583 (intraperitoneal injection; 2 mg/kg) attenuates LPS-induced lung injury, pre-treatment with this compound can significantly decrease LPS-increased IL-6 levels in WT-mice, In contrast, BAY 60-6583 treatment is ineffective in abrogating these inflammatory parameters in  A2BAR−/−  mice[2].
BAY 60-6583 (intratumoral administration) causes a significant increase in tumor-infiltrating MDSCs, it does not affect neither their ability to suppress T-cell proliferation nor their degree of maturation, it also stimulates the production of IL-10 and CCL2 in the tumor tissue[5].

Animal Model:  A2BAR−/−  mice on a C57BL/6J mice[1]
Dosage: 2 mg/kg
Administration: Intraperitoneal injection; 2 mg/kg
Result: Demonstrated attenuation of lung inflammation and pulmonary edema in wild-type but not in gene-targeted mice for the A2BAR.
Molecular Weight

379.44

Formula

C₁₉H₁₇N₅O₂S

CAS No.

910487-58-0

SMILES

O=C(N)CSC1=NC(N)=C(C#N)C(C2=CC=C(OCC3CC3)C=C2)=C1C#N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
References

Purity: >99.0%

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Keywords:

BAY 60-6583Adenosine ReceptorP1 receptorAcute Lung Injurypulmonary edematype 2 diabetesobesitymyocardial ischemiaInhibitorinhibitorinhibit

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BAY 60-6583
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