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MRS1220

Catalog No. T23016   CAS 183721-15-5
Synonyms: MRS 1220

MRS1220, a selective and potent antagonist for the human A3 adenosine receptor (hA3AR) with a dissociation constant (Ki) of 0.59 nM, exhibits therapeutic promise for central nervous system disease research. It effectively diminishes glioblastoma tumor size and inhibits blood vessel formation in vivo.

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MRS1220 Chemical Structure
MRS1220, CAS 183721-15-5
Pack Size Availability Price/USD Quantity
1 mg In stock $ 76.00
5 mg In stock $ 197.00
10 mg In stock $ 313.00
25 mg In stock $ 533.00
50 mg In stock $ 768.00
100 mg In stock $ 1,080.00
500 mg In stock $ 2,160.00
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Purity: 96.59%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description MRS1220, a selective and potent antagonist for the human A3 adenosine receptor (hA3AR) with a dissociation constant (Ki) of 0.59 nM, exhibits therapeutic promise for central nervous system disease research. It effectively diminishes glioblastoma tumor size and inhibits blood vessel formation in vivo.
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].
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].
Synonyms MRS 1220
Molecular Weight 403.82
Formula C21H14ClN5O2
CAS No. 183721-15-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 7.2mg/mL (17.8mM)

TargetMolReferences and Literature

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.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Anti-Cancer Active Compound Library GPCR Compound Library Neurotransmitter Receptor Compound Library Neuronal Signaling Compound Library Bioactive Compound Library Bioactive Compounds Library Max Anti-Cancer Compound Library

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Keywords

MRS1220 183721-15-5 GPCR/G Protein Neuroscience Adenosine Receptor MRS-1220 MRS 1220 inhibitor inhibit

 

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