中文名称: | BAY 60-6583 | ||||
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英文名称: | BAY 60-6583 | ||||
别名: | BAY 60-6583;2-[6-amino-3,5-dicyano-4-[4-(cyclopropylmethoxy)phenyl]pyridin-2-yl]sulfanylacetamide | ||||
CAS No: | 910487-58-0 | 分子式: | C19H17N5O2S | 分子量: | 379.44 |
CAS No: | 910487-58-0 | ||||
分子式: | C19H17N5O2S | ||||
分子量: | 379.44 |
基本信息
产品编号: |
B10826 |
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产品名称: |
BAY 60-6583 |
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CAS: |
910487-58-0 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
6个月 |
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分子量: |
379.44 |
-20℃ |
1个月 |
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化学名: |
2-[6-amino-3,5-dicyano-4-[4-(cyclopropylmethoxy)phenyl]pyridin-2-yl]sulfanylacetamide |
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Solubility (25°C): |
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体外:
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DMSO |
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Ethanol |
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Water |
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体内(现配现用): |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
2.6355mL |
13.1773mL |
26.3546mL |
5mM |
0.5271mL |
2.6355mL |
5.2709mL |
10mM |
0.2635mL |
1.3177mL |
2.6355mL |
生物活性
产品描述 |
一种腺苷A2B受体的高效选择性激动剂,对A2B受体 (EC50=3nM)的选择性高于A1,A2A和A3受体。BAY 60-6583可以与小鼠,兔和狗A2BAR 结合,Ki值分别为750nM,340nM和330 nM。BAY 60-6583在心肌缺血模型中具有心脏保护作用。 |
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靶点 |
Adenosine Receptor |
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体外研究 |
BAY 60-6583 exhibits EC50 values for receptor activation >10,000nM for both A1 and A2A AR and 3nM for A2B AR subtype in CHO cells expressing recombinant human A1,A2A or A2B ARs.BAY 60-6583(0-10µM) 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 500nM 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±19nM,respectively,in T24 cells.BAY 60-6583 (5μM;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 (5μM;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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Cell Cycle Analysis |
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Cell Line: |
RAW264.7 preosteoclasts |
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Concentration: |
5μM |
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Incubation Time: |
48 hours |
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Result: |
Caused an arrest of cells at the G1 phase. |
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Western Blot Analysis |
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Cell Line: |
RAW264.7 preosteoclasts |
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Concentration: |
5μM |
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Incubation Time: |
48 hours |
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Result: |
Exhibited an inhibition of M-CSF-mediated Akt activation and resulted in the decrease of osteoclast proliferation. |
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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;2mg/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. |
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Animal Model: |
A2BAR−/− mice on a C57BL/6J mice |
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Dosage: |
2mg/kg |
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Administration: |
Intraperitoneal injection;2mg/kg |
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Result: |
Demonstrated attenuation of lung inflammation and pulmonary edema in wild-type but not in gene-targeted mice for the A2BAR. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )