| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
T35539-5mg买3赠1 |
96.00% | ￥654.00 |
6 | - | - | - | - |
|
T35539-10mg买3赠1 |
96.00% | ￥824.00 |
6 | - | - | - | - |
|
T35539-25mg买3赠1 |
96.00% | ￥1640.00 |
6 | - | - | - | - |
|
T35539-100mg |
≥95% | ￥4310.00 |
货期：3-5天 | - | - | - | - |
|
| 产品描述： | BAY 60-6583 是腺苷 A2B受体 的高效选择性激动剂， 对 A2B 受体 (EC50= 3 nM) 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 750 nM，340 nM 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： | AdenosineReceptor | ||||||||||||||||||||
| 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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| 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. |
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| 参考文献： | 1. Aherne CM, et al. Epithelial-specific A2B adenosine receptor signaling protects the colonic epithelial barrier during acute colitis.Mucosal Immunol. 2015 Nov;8(6):1324-38. 2. Schingnitz U, et al. Signaling through the A2B adenosine receptor dampens endotoxin-induced acute lung injury.J Immunol. 2010 May 1;184(9):5271-9. 3. Gao ZG, et al. Probing biased/partial agonism at the G protein-coupled A(2B) adenosine receptor.Biochem Pharmacol. 2014 Aug 1;90(3):297-306. 4. Yoon Taek Oh, et al. A2B Adenosine Receptor Stimulation Down-regulates M-CSF-mediated Osteoclast Proliferation. Biomed Sci Letters 2017;23:194-200 5. John A. Auchampach, et al. Characterization of the A2B Adenosine Receptor from Mouse, Rabbit, and Dog. J Pharmacol Exp Ther. 2009 Apr;329(1):2-13. 6. Morello S1, et al. Targeting the adenosine A2b receptor in the tumor microenvironment overcomes local immunosuppression by myeloid-derived suppressor cells.Oncoimmunology. 2014 Feb 14;3:e27989. eCollection 2014. |
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| 溶解性： | soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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