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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)
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
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
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
E Ongini et al.
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
Elise M Weerts et al.
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
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