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BAY 60-6583

CAS No. : 910487-58-0

MCE 站：BAY 60-6583

产品活性：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，K_i 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。

研究领域：GPCR/G Protein

作用靶点：Adenosine Receptor

In Vitro: 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 ?M) 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.

In Vivo: 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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