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化驗
≥98% (HPLC)
品質等級
形狀
solid
顏色
white
溶解度
DMSO: >10 mg/mL
H2O: insoluble
儲存溫度
room temp
SMILES 字串
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 密鑰
MSJODEOZODDVGW-UHFFFAOYSA-N
基因資訊
human ... ADORA1(134) , ADORA2A(135) , ADORA2B(136) , ADORA3(140)
rat ... Adora1(29290) , Adora2a(25369) , Adora2b(29316)
應用
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.
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
個人防護裝備
Eyeshields, Gloves, type N95 (US)
The Journal of pharmacology and experimental therapeutics, 241(2), 415-420 (1987-05-01)
CGS 15943A, a triazoloquinazoline, is a potent and selective adenosine receptor antagonist as assessed by its effects on radioligand binding and adenosine-stimulated adenylate cyclase activity in guinea pig synaptoneurosomes. At the adenosine A-1 receptor labeled with [3H]cyclohexyladenosine, CGS 15943A had
American journal of physiology. Heart and circulatory physiology, 280(5), H2329-H2335 (2001-04-12)
The purpose of this study was to investigate the receptor subtypes that mediate the dilation of rat intracerebral arterioles elicited by adenosine. Penetrating arterioles were isolated from the rat brain, cannulated with the use of a micropipette system, and luminally
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
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