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M228 Sigma

MRS 1220

solid

Synonym: 9-Chloro-2-(2-furanyl)-5-((phenylacetyl)amino)-[1,2,4]triazolo[1,5-c]quinazoline

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Properties

Related Categories Adenosines/P2 Nucleotide Receptor - Antagonists, Adenosines/P2 Nucleotide Receptors (Purinergics), Antagonists, Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules,
InChI Key   TWWFAXQOKNBUCR-UHFFFAOYSA-N
form   solid
color   white
solubility   DMSO: soluble2 mg/mL
  2-hydroxypropyl-β-cyclodextrin: insoluble
  H2O: insoluble
  ethanol: insoluble
Gene Information   human ... ADORA3(140)
rat ... Adora1(29290), Adora2a(25369), Adora3(25370)

Description

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.

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Documents

Certificate of Analysis

Protocols & Articles

Articles

Fluorescent G protein-coupled receptors (GPCRs)

G protein-coupled receptors (GPCRs) are the largest class of transmembrane proteins and the targets for almost half of the clinical drugs in the market today. Advances in X-ray crystallography and ot...
Mike Earley, Market Segment Manager, Sigma Life Science
Biofiles Vol. 8, No. 4
Keywords: Clinical, Confocal microscopy, Ligands, Microscopy

Peer-Reviewed Papers
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