BAY 60-6583

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BAY 60-6583 (BAY606583) 是一种有效的选择性腺苷 A2B 受体激动剂，EC50 为 2.83 nM。

BAY 60-6583 (BAY606583) is a potent, selective adenosine A2B receptor agonist with EC50 of 2.83 nM (murine A2BR); inhibits fMLP-stimulated superoxide production by either naive neutrophils,TNF-α-primed neutrophils, or neutrophils isolated from mice at 1-10 nM; increases fMLP-stimulated superoxide production at higher concentrations (>1 uM); exhibits cardioprotective activity, attenuates infarct size in mouse model of myocardial ischemia.

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.?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.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.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. Cell Cycle Analysis 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 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.

BAY 60-6583 (intravenous injection; 100 mcg/kg) reduces the infarction area just prior to reperfusion in ischaemic rabbit hearts.?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, 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. Animal Model:?A2BAR?/? ?mice on a C57BL/6J mice 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.

BAY606583

Apoptosis

Adenosine Receptor

Adenosine Receptor

——

——

910487-58-0

379.438

C19H17N5O2S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (263.55 mM)

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

2-[[6-Amino-3,5-dicyano-4-[4-(cyclopropylmethoxy)phenyl]-2-pyridinyl]thio]acetamide

(-20℃)

With Ice Pack

≥ 2 years