1. GPCR/G Protein
  2. Adenosine Receptor
  3. MRS1220

MRS1220 

Cat. No.: HY-103190
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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. MRS1220 reduces glioblastoma tumor size and blood vessel formation in vivo.

For research use only. We do not sell to patients.

MRS1220 Chemical Structure

MRS1220 Chemical Structure

CAS No. : 183721-15-5

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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].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

403.82

Formula

C₂₁H₁₄ClN₅O₂

CAS No.
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MRS1220
Cat. No.:
HY-103190
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