质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: 20 mg/mL, clear
储存温度
2-8°C
SMILES字符串
NC1=C(C#N)C(C2=CC=C(OCC3CC3)C=C2)=C(C#N)C(SCC(N)=O)=N1
InChI
1S/C19H17N5O2S/c20-7-14-17(12-3-5-13(6-4-12)26-9-11-1-2-11)15(8-21)19(24-18(14)23)27-10-16(22)25/h3-6,11H,1-2,9-10H2,(H2,22,25)(H2,23,24)
InChI key
ZTYHZMAZUWOXNC-UHFFFAOYSA-N
生化/生理作用
BAY 60-6583是一种有效的腺苷受体A2b（A2bR）的部分激动剂（抑制0.3 nM [3H] PSB-603与人/小鼠/大鼠A2bR结合的Ki = 114/136/100 nM），可在转染后表达人A2bR（EC50〜100 nM）的CHO中选择性诱导cAMP依赖性转录活性，但在表达A1R或A2aR的CHO中无效，其对人/大鼠/小鼠A2aR没有亲和力。BAY 60-6583还显示出对A1R（抑制1 nM [3H]CCPA与人/小鼠/大鼠A1R结合的 Ki= 387/351/514 nM；对100 nM CCPA诱导的hA1R β-抑制蛋白募集过程的抑制IC50 = 7.4 μM）和A3R（抑制10 nM [3H]NECA与人/小鼠/大鼠的A3R结合的 Ki= 223/3920/2750 nM；对30 nM Cl-IB-MECA诱导的hA3R β-抑制蛋白募集过程的抑制IC50 = 6.7 μM）的低亲和性拮抗活性。BAY 60-6583已通过i.p.（0.1-80 mg/kg）或i.v.（0.2-2 mg/kg）广泛应用于动物体内，以研究A2bR介导的生物反应。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Atsushi Kuno et al.
Journal of molecular and cellular cardiology, 43(3), 262-271 (2007-07-17)
Although protein kinase C (PKC) plays a key role in ischemic preconditioning (IPC), the actual mechanism of that protection is unknown. We recently found that protection from IPC requires activation of adenosine receptors during early reperfusion. We, therefore, hypothesized that
Tobias Eckle et al.
Circulation, 115(12), 1581-1590 (2007-03-14)
Ecto-5'-nucleotidase (CD73)-dependent adenosine generation has been implicated in tissue protection during acute injury. Once generated, adenosine can activate cell-surface adenosine receptors (A1 AR, A2A AR, A2B AR, A3 AR). In the present study, we define the contribution of adenosine to
Mohamad Wessam Alnouri et al.
Purinergic signalling, 11(3), 389-407 (2015-07-02)
Adenosine receptors (ARs) have emerged as new drug targets. The majority of data on affinity/potency and selectivity of AR ligands described in the literature has been obtained for the human species. However, preclinical studies are mostly performed in mouse or
Vanessa D'Antongiovanni et al.
Cells, 9(5) (2020-05-24)
The role played by adenosine A2B receptors (A2BRs) in the regulation of enteric glial cell (EGC) functions remains unclear. This study was aimed at investigating the involvement of A2BRs in the control of EGC functions in a model of obesity.
Francesco Cilenti et al.
Immunity, 54(8), 1665-1682 (2021-06-16)
Tight control of inflammatory gene expression by antagonistic environmental cues is key to ensure immune protection while preventing tissue damage. Prostaglandin E2 (PGE2) modulates macrophage activation during homeostasis and disease, but the underlying mechanisms remain incompletely characterized. Here we dissected
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