产品
编 号：F515936
分子式：C19H17N5O2S
分子量：379.44
分子式：C19H17N5O2S
分子量：379.44
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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50mg
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100mg
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结构图
CAS No: 910487-58-0
产品详情
生物活性：
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.
体内研究：
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, In contrast, BAY 60-6583 treatment is ineffective in abrogating these inflammatory parameters in ?A2BAR?/? ?mice.?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.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.
体外研究：
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.
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.
体内研究：
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, In contrast, BAY 60-6583 treatment is ineffective in abrogating these inflammatory parameters in ?A2BAR?/? ?mice.?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.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.
体外研究：
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.
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