MRS 1220

Cat. No. 1217

MRS 1220 C21H14ClN5O2 [183721-15-5]

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Chemical Name: N-[9-Chloro-2-(2-furanyl)[1,2,4]-triazolo[1,5-c]quinazolin-5-yl]benzene acetamide

Biological Activity

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).

Licensing Information

Sold with the permission of the NIH, US Patent 60/029,855

Technical Data

M.Wt:
403.83
Formula:
C21H14ClN5O2
Solubility:
Soluble to 100 mM in DMSO with gentle warming
Purity:
>98 %
Storage:
Store at RT
CAS No:
183721-15-5

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

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.

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.

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Citations are publications that use Tocris products. Selected citations for MRS 1220 include:

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.

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.

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.

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.

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.

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.

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Keywords: MRS 1220, supplier, potent, selective, hA3, antagonists, Receptors, adenosines, MRS1220, Tocris Bioscience, Adenosine A3 Receptor Antagonist products

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