MRS1220 是一种高效、选择性的人 A3 腺苷受体 (hA3AR) 拮抗剂，Ki 为 0.59 nM，可用于中枢神经系统疾病的研究。MRS1220 在体内还减少了胶质母细胞瘤的肿瘤大小和血管形成。

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[1]. VEGF secretion in U87MG glioblastoma stem-like cells (GSCs) decreases ~25% with MRS1220 after 72 h of hypoxia[2].

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].

183721-15-5

C21H14ClN5O2

403.82

MRS 1220

DMSO:7.2mg/mL (17.8mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years