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BAY 60-6583

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Chemical Structure| 910487-58-0 同义名 : -
CAS号 : 910487-58-0
货号 : A818008
分子式 : C19H17N5O2S
纯度 : 98%
分子量 : 379.436
MDL号 : MFCD22683833
存储条件:

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(276.73 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
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
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

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.