MRS 1220

Names

[ Name ]:
MRS 1220

[Synonym ]:
MRS 1220
9-Chloro-2-(2-furanyl)-5-((phenylacetyl)amino)-[1,2,4]triazolo[1,5-c]quinazoline
Tocris-1217
MFCD01321046

Biological Activity

[Description]:

MRS1220, a highly potent and selective human A3 adenosine receptor (hA3AR) antagonist with a Ki of 0.59 nM, has therapeutic potential for the research of diseases of the central nervous system[1]. MRS1220 reduces glioblastoma tumor size and blood vessel formation in vivo[2].

[Related Catalog]:

Research Areas >> Cancer

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> Adenosine Receptor

[In Vitro]

MRS 1220 reverses the effect of A3 agonist-elicited inhibition of tumor necrosis factor-α formation in the human macrophage U-937 cell line with an IC50 of 0.3 μM[1]. VEGF secretion in U87MG glioblastoma stem-like cells (GSCs) decreases ~25% with MRS1220 after 72 h of hypoxia[2]. Cell Viability Assay[2] Cell Line: U87MG GSCs Concentration: 10 μM Incubation Time: 72 hours Result: Decreased ~25% VEGF secretion.

[In Vivo]

MRS1220 (0.15 mg/kg; intraperitoneal inoculation) reduces tumor size and blood vessel formation in vivo. MRS1220 exhibits a strong in vivo anti-angiogenic effect[2]. Animal Model: Eight, 8 week-old male Sprague-Dawley rats bearing C6 (GSCs)[2] Dosage: 0.15 mg/kg/72 h Administration: Administered by intraperitoneal inoculation, for fifteen days Result: A reduction close to 80% and 90% in tumor volume compared to the vehicle-treated group at day ten and fifteen post-treatment, respectively.

[References]

[1]. K A Jacobson, et al. Pharmacological characterization of novel A3 adenosine receptor-selective antagonists. Neuropharmacology. 1997 Sep;36(9):1157-65.

[2]. René Rocha, et al. The Adenosine A₃ Receptor Regulates Differentiation of Glioblastoma Stem-Like Cells to Endothelial Cells under Hypoxia. Int J Mol Sci. 2018 Apr 18;19(4):1228.

Chemical & Physical Properties

[ Density]:
1.49g/cm3

[ Molecular Formula ]:
C₂₁H₁₄ClN₅O₂

[ Molecular Weight ]:
403.82

[ Exact Mass ]:
403.08400

[ PSA ]:
85.32000

[ LogP ]:
4.44510

[ Index of Refraction ]:
1.744

MSDS

Click to get detail MSDS

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
3

Articles

Fragment-Based Discovery of Subtype-Selective Adenosine Receptor Ligands from Homology Models.

J. Med. Chem. 58 , 9578-90, (2015)

Fragment-based lead discovery (FBLD) holds great promise for drug discovery, but applications to G protein-coupled receptors (GPCRs) have been limited by a lack of sensitive screening techniques and s...

Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype.

J. Med. Chem. 39 , 4142-4148, (1996)

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 recept...

Pharmacological characterization of novel A3 adenosine receptor-selective antagonists.

Neuropharmacology 36 , 1157-1165, (1997)

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 triazoloquinazolin...