MRS 1220
Chemical Name: N-[9-Chloro-2-(2-furanyl)[1,2,4]-triazolo[1,5-c]quinazolin-5-yl]benzene acetamide
Purity: ≥98%
Biological Activity
MRS 1220 is a potent and highly selective antagonist at the human A3 adenosine receptor (Ki values are 0.65, 305, and 52 nM at hA3, rA1 and rA2A respectively. Displays an IC50 value > 1 μM for inhibition of binding to rat A3 receptors).Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
Fox JT, Sakamuru S, Huang R
Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8. -
Ability of ?? T cells to modulate the Foxp3 T cell response is dependent on adenosine
D Liang, JI Woo, H Shao, WK Born, RL O'Brien, HJ Kaplan, D Sun
PLoS ONE, 2018;13(5):e0197189. -
Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) are selective for the human A3 receptor subtype.
Kim et al.
J.Med.Chem., 1996;39:4142 -
Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) having high potency at the human A2B and A3 receptor subtypes.
Kim et al.
J.Med.Chem., 1998;41:2835 -
Pharmacological characterization of novel A3 adenosine receptor selective antagonists.
Jacobson et al.
Neuropharmacology, 1997;36:1157
Product Datasheets
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Citations for MRS 1220
The citations listed below are publications that use Tocris products. Selected citations for MRS 1220 include:
13 Citations: Showing 1 - 10
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Anti-Depressant Flu Reveals its Therapeutic Effect Via Astrocytes.
Authors: Kinoshita Et al.
EBioMedicine 2018;32:72
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Adenosine binds predominantly to adenosine receptor A1 subtype in astrocytes and mediates an immunosuppressive effect.
Authors: Liu Et al.
Brain Res 2018;1700:47
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Adenosine A3 receptor elicits chemoresistance mediated by multiple resistance-associated protein-1 in human glioblastoma stem-like cells.
Authors: Torres Et al.
Oncotarget 2016;7:67373
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Neuropharmacology of purinergic receptors in human submucous plexus: Involvement of P2X?, P2X?, P2X? channels, P2Y and A? metabotropic receptors in neurotransmission.
Authors: Liñán-Rico Et al.
Neuropharmacology 2015;95:83
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Application of BRET to monitor ligand binding to GPCRs.
Authors: Stoddart Et al.
Nat Methods 2015;12:661
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Kinetic analysis of antagonist-occupied adenosine-A3 receptors within membrane microdomains of individual cells provides evidence of receptor dimerization and allosterism.
Authors: Corriden Et al.
FASEB J 2014;28:4211
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Characterization by flow cytometry of fluorescent, selective agonist probes of the A(3) adenosine receptor.
Authors: Kozma Et al.
Biochem Pharmacol 2013;85:1171
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Fragment screening at adenosine-A(3) receptors in living cells using a fluorescence-based binding assay.
Authors: Stoddart Et al.
Chem Biol 2012;19:1105
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Adenosine receptor regulation of coronary blood flow in Ossabaw miniature swine.
Authors: Long Et al.
Am J Physiol Gastrointest Liver Physiol 2010;335:781
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A3 adenosine receptor antagonists delay irreversible synaptic failure caused by oxygen and glucose deprivation in the rat CA1 hippocampus in vitro.
Authors: Pugliese Et al.
Br J Pharmacol 2006;147:524
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Characterization of ERK1/2 signalling pathways induced by adenosine receptor subtypes in newborn rat cardiomyocytes.
Authors: Germack and Dickenson
Br J Pharmacol 2004;141:329
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Extracellular ATP and adenosine induce cell apoptosis of human hepatoma Li-7A cells via the A3 adenosine receptor.
Authors: Wen and Knowles
Br J Pharmacol 2003;140:1009
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Alteration of the purinergic modulation of enteric neurotransmission in the mouse ileum during chronic intestinal inflammation.
Authors: Man Et al.
Br J Pharmacol 2003;139:172
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