产品
编 号:F229964
分子式:C21H14ClN5O2
分子量:403.82
产品类型
结构图
CAS No: 183721-15-5
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产品详情
生物活性:
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.
体内研究:
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.
体外研究:
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.