BAY 60-6583 is a potent and high affinity adenosine A2B receptor agonist at A1, A2A and A3 receptors with an EC50 value of 3 nM. 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 exhibits a cardioprotective effect in myocardial ischemia models [1][5].In CHO cells expressing recombinant human A1, A2A or A2B ARs, BAY 60-6583 showed receptor activation EC50 values greater than 10,000 nM for A1 and A2A ARs, and 3 nM for A2B AR isoforms[1] .The maximum agonistic effect of BAY 60-6583 was 68% in the concentration range of 0-10 μM. In T24 cells, the EC50 values of BAY 60-6583 were 98±22, 102±17, 127±31 and 93±19 nM, respectively[3] .At a concentration of 5 μM, BAY 60-6583 acted for 24 h to increase the accumulation of G1-phase cells and decrease the accumulation of G2/M-phase cells in RAW264.7 preosteoclasts.BAY 60-6583 specifically inhibited the activation of Akt by M-CSF without affecting the M-CSF-induced activation of ERK1/2[4].
BAY 60-6583 动物研究
Animal study
Administered intravenously at a dose of 100 mcg/kg, BAY 60-6583 reduces infarct size before reperfusion in ischemic rabbit hearts[1] .Administered at a dose of 2 mg/kg, intraperitoneally, BAY 60-6583 attenuated LPS-induced lung injury. In contrast, BAY 60-6583 was not effective in alleviating inflammatory indices in A2BAR-/- mice[2].BAY 60-6583 (intratumoural administration) leads to a significant increase in tumour-infiltrating MDSCs, but neither affects their ability to inhibit T-cell proliferation nor their maturation, and it stimulates the production of IL-10 and CCL2 in tumour tissue [5].
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