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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).
Sold with the permission of the NIH, US Patent 60/029,855
|Storage||Store at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|DMSO||8.08||20 with gentle warming|
Preparing Stock Solutions
The following data is based on the product molecular weight 403.83. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.2 mM||12.38 mL||61.91 mL||123.81 mL|
|1 mM||2.48 mL||12.38 mL||24.76 mL|
|2 mM||1.24 mL||6.19 mL||12.38 mL|
|10 mM||0.25 mL||1.24 mL||2.48 mL|
References are publications that support the biological activity of the product.
Jacobson et al (1997) Pharmacological characterization of novel A3 adenosine receptor selective antagonists. Neuropharmacology 36 1157 PMID: 9364471
Kim et al (1996) Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) are selective for the human A3 receptor subtype. J.Med.Chem. 39 4142 PMID: 8863790
Kim et al (1998) Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) having high potency at the human A2B and A3 receptor subtypes. J.Med.Chem. 41 2835 PMID: 9667972
If you know of a relevant reference for MRS 1220, please let us know.
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Keywords: MRS 1220, MRS 1220 supplier, potent, selective, hA3, antagonists, Receptors, adenosines, MRS1220, Adenosine, A3, 1217, Tocris Bioscience
12 Citations for MRS 1220
Citations are publications that use Tocris products. Selected citations for MRS 1220 include:
Liu et al (2018) Adenosine binds predominantly to adenosine receptor A1 subtype in astrocytes and mediates an immunosuppressive effect. Brain Res 1700 47 PMID: 29935155
Stoddart et al (2015) Application of BRET to monitor ligand binding to GPCRs. Nat Methods 12 661 PMID: 26030448
Corriden et al (2014) Kinetic analysis of antagonist-occupied adenosine-A3 receptors within membrane microdomains of individual cells provides evidence of receptor dimerization and allosterism. FASEB J 28 4211 PMID: 24970394
Long et al (2010) Adenosine receptor regulation of coronary blood flow in Ossabaw miniature swine. Am J Physiol Gastrointest Liver Physiol 335 781 PMID: 20855445
Stoddart et al (2012) Fragment screening at adenosine-A(3) receptors in living cells using a fluorescence-based binding assay. Chem Biol 19 1105 PMID: 22999879
Pugliese et al (2006) A3 adenosine receptor antagonists delay irreversible synaptic failure caused by oxygen and glucose deprivation in the rat CA1 hippocampus in vitro. Br J Pharmacol 147 524 PMID: 16415905
Torres et al (2016) Adenosine A3 receptor elicits chemoresistance mediated by multiple resistance-associated protein-1 in human glioblastoma stem-like cells. Oncotarget 7 67373 PMID: 27634913
Germack and Dickenson (2004) Characterization of ERK1/2 signalling pathways induced by adenosine receptor subtypes in newborn rat cardiomyocytes. Br J Pharmacol 141 329 PMID: 14751870
Man et al (2003) Alteration of the purinergic modulation of enteric neurotransmission in the mouse ileum during chronic intestinal inflammation. Br J Pharmacol 139 172 PMID: 12746236
Wen and Knowles (2003) Extracellular ATP and adenosine induce cell apoptosis of human hepatoma Li-7A cells via the A3 adenosine receptor. Br J Pharmacol 140 1009 PMID: 14530217
Liñán-Rico et al (2015) Neuropharmacology of purinergic receptors in human submucous plexus: Involvement of P2X?, P2X?, P2X? channels, P2Y and A? metabotropic receptors in neurotransmission. Neuropharmacology 95 83 PMID: 25724083
Kozma et al (2013) Characterization by flow cytometry of fluorescent, selective agonist probes of the A(3) adenosine receptor. Biochem Pharmacol 85 1171 PMID: 23376019
Do you know of a great paper that uses MRS 1220 from Tocris? Please let us know.
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