生物活性 | |||
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描述 | 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]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.64mL 0.53mL 0.26mL |
13.18mL 2.64mL 1.32mL |
26.35mL 5.27mL 2.64mL |
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