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方案
≥98% (HPLC)
质量水平
表单
solid
颜色
white
溶解性
DMSO: >10 mg/mL
H2O: insoluble
储存温度
room temp
SMILES字符串
Nc1nc2ccc(Cl)cc2c3nc(nn13)-c4ccco4
InChI
1S/C13H8ClN5O/c14-7-3-4-9-8(6-7)12-17-11(10-2-1-5-20-10)18-19(12)13(15)16-9/h1-6H,(H2,15,16)
InChI key
MSJODEOZODDVGW-UHFFFAOYSA-N
基因信息
human ... ADORA1(134) , ADORA2A(135) , ADORA2B(136) , ADORA3(140)
rat ... Adora1(29290) , Adora2a(25369) , Adora2b(29316)
应用
CGS-15943 has been used as a non-selective adenosine receptor antagonist to study its effects on the proliferation of pancreatic ductal adenocarcinoma (PDAC) cells and hepatocellular carcinoma (HCC). It has also been used as a non-selective adenosine receptor antagonist to investigate the mechanism underlying adenosine inhibition on cholangiocarcinoma (CCA) cells.
生化/生理作用
CGS-15943 is a potent and non-selective adenosine receptor antagonist. It exhibits anti-carcinogenic and anti-apoptotic activity.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
Eyeshields, Gloves, type N95 (US)
从最新的版本中选择一种:
分析证书(COA)
Psychopharmacology, 168(1-2), 155-163 (2003-04-02)
Caffeine and the adenosine A(1) and A(2A) receptor antagonist CGS15943 produce many behavioral effects that are similar to those produced by classic stimulant drugs (e.g. cocaine and amphetamines). The current study evaluated whether CGS15943 would maintain self-administration and reinstate extinguished
The Journal of surgical research, 80(2), 357-364 (1999-01-08)
Adenosine is a potent vasodilator of vascular smooth muscle. Endothelium-derived nitric oxide (NO) elicits vasodilation. We have previously reported that adenosine stimulates the production of NO from porcine carotid arterial endothelial cells (PCAEC) via a receptor-mediated mechanism. This study was
Modeling the adenosine receptors: comparison of the binding domains of A2A agonists and antagonists.
Journal of medicinal chemistry, 46(23), 4847-4859 (2003-10-31)
A three-dimensional model of the human A(2A) adenosine receptor (AR) and its docked ligands was built by homology to rhodopsin and validated with site-directed mutagenesis and the synthesis of chemically complementary agonists. Different binding modes of A(2A)AR antagonists and agonists
The Journal of biological chemistry, 277(40), 37124-37130 (2002-07-30)
We investigated the effects of methylxanthines on enzymatic activity of phosphoinositide 3-kinases (PI3Ks). We found that caffeine inhibits the in vitro lipid kinase of class I PI3Ks (IC(50) = 75 microm for p110 delta, 400 microm for p110 alpha and
Naunyn-Schmiedeberg's archives of pharmacology, 359(1), 7-10 (1999-02-05)
Three structurally related non-xanthine compounds, CGS 15943, ZM 241385 and SCH 58261, are potent A2A adenosine receptor antagonists and have been used as tools in many pharmacological studies. We have now characterized their affinity and selectivity profile on human adenosine
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