BAY 60-6583  ≥98%

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包装规格:1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
产品简介: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。
溶解性:溶于DMSO(20mg/mL)
储备液保存:-80°C, 2 years -20°C, 1 year
体内实验:1、请依序添加每种溶剂: 10% DMSO→40% PEG300→5% Tween-80→45% Saline Solubility: ≥ 4.17 mg/mL (10.99 mM); 澄清溶液 此方案可获得 ≥ 4.17 mg/mL(饱和度未知)的澄清溶液。 以 1 mL 工作液为例,取 100 μL 41.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL。 2、请依序添加每种溶剂: 10% DMSO→90% Corn Oil Solubility: ≥ 4.17 mg/mL (10.99 mM); 澄清溶液 此方案可获得 ≥ 4.17 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。 以 1 mL 工作液为例,取 100 μL 41.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 <1mg/ml表示微溶或不溶。 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。 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。
体外研究:BAY 60-6583 exhibitsEC50 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.
体内研究:BAY 60-6583 (intravenousinjection; 100 mcg/kg) reduces the infarction area just prior to reperfusion in ischaemic rabbit hearts. BAY 60-6583 (intraperitonealinjection; 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 A2BARmice. 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.
保存条件:-20℃
注意事项:1、为了您的安全和健康,请穿实验服并戴一次性手套操作。 2、以上信息仅做参考交流之用。