MRS1220

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

MRS1220 

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[1]< /sup>。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

MRS1220 Chemical Structure

CAS No. : 183721-15-5

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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[1]. MRS1220 reduces glioblastoma tumor size and blood vessel formation in vivo[2].

体外研究
(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].

上海金畔生物科技有限公司 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.

体内研究
(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].

上海金畔生物科技有限公司 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.

分子量

403.82

Formula

C21H14ClN5O2
CAS 号

183721-15-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [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.

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