MRS1220

Research use only, not for human use.

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.

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.

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.VEGF secretion in U87MG glioblastoma stem-like cells (GSCs) decreases ~25% with MRS1220 after 72 h of hypoxia.Cell Viability Assay Cell Line:U87MG GSCs Concentration:10 μM Incubation Time:72 hours Result:Decreased ~25% VEGF secretion.

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.Animal Model:Eight, 8 week-old male Sprague-Dawley rats bearing C6 (GSCs) 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.

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GPCR/G Protein

Adenosine Receptor

Adenosine Receptor

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183721-15-5

403.82

C21H14ClN5O2

>98% (HPLC)

In Vitro:?DMSO : 4 mg/mL (9.91 mM; Ultrasonic (<60°C)

Clc1ccc2nc(NC(=O)Cc3ccccc3)n3nc(nc3c2c1)-c1ccco1

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(-20℃)

With Ice Pack

≥ 2 years