M228
MRS 1220
solid
别名:
9-Chloro-2-(2-furanyl)-5-((phenylacetyl)amino)-[1,2,4]triazolo[1,5-c]quinazoline
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关于此项目
经验公式（希尔记法）:
C21H14ClN5O2
化学文摘社编号:
分子量:
403.82
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352209
MDL number:
Form:
solid
Quality level:
产品名称
MRS 1220, solid
InChI
1S/C21H14ClN5O2/c22-14-8-9-16-15(12-14)20-25-19(17-7-4-10-29-17)26-27(20)21(23-16)24-18(28)11-13-5-2-1-3-6-13/h1-10,12H,11H2,(H,23,24,28)
SMILES string
Clc1ccc2nc(NC(=O)Cc3ccccc3)n4nc(nc4c2c1)-c5ccco5
InChI key
TWWFAXQOKNBUCR-UHFFFAOYSA-N
form
solid
color
white
solubility
DMSO: 2 mg/mL
2-hydroxypropyl-β-cyclodextrin: insoluble
H2O: insoluble
ethanol: insoluble
Quality Level
Gene Information
human ... ADORA3(140)
rat ... Adora1(29290), Adora2a(25369), Adora3(25370)
Biochem/physiol Actions
MRS1220 is a putative A3 adenosine receptor antagonist. MRS 1220 was found to be competitive in saturation binding studies using the agonist radioligand 125I AB-MECA at cloned human brain A3 receptors expressed in HEK-293 cells. Antagonism was demonstrated in functional assays consisting of agonist-induced inhibition of adenylate cyclase and the stimulation of binding of 35S guanosine 5′-O-(3-thiotriphosphate (35S GTP-gamma-S) to the associated G-proteins. MRS 1220 and MRS 1191, with KB values of 1.7 and 92 nM, respectively, proved to be highly selective for human A3 receptor vs human A1 receptor-mediated effects on adenylate cyclase. In addition, MRS 1220 reversed the effect of A3 agonist-elicited inhibition of tumor necrosis factor-alpha formation in the human macrophage U-937 cell line, with an IC50 value of 0.3 μM.
Features and Benefits
This compound is featured on the Adenosine Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
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)
Pnina Fishman et al.
Arthritis research & therapy, 8(1), R33-R33 (2006-03-02)
The anti-inflammatory effect of adenosine was previously found to be mediated via activation of the A3 adenosine receptor (A3AR). The aim of the present study was to decipher the molecular mechanism involved with the inhibitory effect of IB-MECA, an A3AR
Naunyn-Schmiedeberg'S Archives of Pharmacology, 364, 225-234 (2000)
Seyyed Mehdi Jafari et al.
Journal of cellular biochemistry, 118(9), 2909-2920 (2017-02-24)
Numerous studies have demonstrated the role of A3 adenosine receptor (A3AR) and signaling pathways in the multiple aspects of the tumor. However, there is a little study about the function of A3AR in the biological processes of cancer stem cells
Y C Kim et al.
Journal of medicinal chemistry, 39(21), 4142-4148 (1996-10-11)
The adenosine antagonist 9-chloro-2-(2-furanyl)[1,2,4]triazolo[1,5-c]quinazolin-5-amine (CGS15943) binds to human A3 receptors with high affinity (Ki = 14 nM), while it lacks affinity at rat A3 receptors. Acylated derivatives of the 5-amino group and other modifications were prepared in an effort to
K A Jacobson et al.
Neuropharmacology, 36(9), 1157-1165 (1997-11-19)
The effects of putative A3 adenosine receptor antagonists of three diverse chemical classes (the flavonoid MRS 1067, the 6-phenyl-1,4-dihydropyridines MRS 1097 and MRS 1191, and the triazoloquinazoline MRS 1220) were characterized in receptor binding and functional assays. MRS1067, MRS 1191
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