C199
CGS-15943
≥98% (HPLC), Adenosine receptor antagonist, solid
别名:
9-Chloro-2-(2-furanyl)-[1,2,4]triazolo[1,5-c]quinazolin-5-amine
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关于此项目
经验公式（希尔记法）:
C13H8ClN5O
化学文摘社编号:
分子量:
285.69
UNSPSC Code:
12352202
PubChem Substance ID:
NACRES:
NA.77
MDL number:
产品名称
CGS-15943, solid
SMILES string
Nc1nc2ccc(Cl)cc2c3nc(nn13)-c4ccco4
InChI key
MSJODEOZODDVGW-UHFFFAOYSA-N
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)
assay
≥98% (HPLC)
form
solid
color
white
solubility
DMSO: >10 mg/mL
H2O: insoluble
storage temp.
room temp
Quality Level
Gene Information
human ... ADORA1(134), ADORA2A(135), ADORA2B(136), ADORA3(140)
rat ... Adora1(29290), Adora2a(25369), Adora2b(29316)
Application
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.
Biochem/physiol Actions
CGS-15943 is a potent and non-selective adenosine receptor antagonist. It exhibits anti-carcinogenic and anti-apoptotic activity.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
A C Ngai et al.
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
M Williams et al.
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
Lazaros C Foukas et al.
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
Modeling the adenosine receptors: comparison of the binding domains of A2A agonists and antagonists.
Soo-Kyung Kim et al.
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
J m Li et al.
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
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