货号	规格	价格	上海	北京	珠海	重庆	武汉
T77865-1mg买3赠1	99.20%	￥490.00 T77865-1mg ￥490.00 现货（买3赠1）	9 9	-	-	-	-
T77865-5mg买3赠1	99.20%	￥1180.00 T77865-5mg ￥1180.00 现货（买3赠1）	7 7	-	-	-	-
T77865-25mg买3赠1	99.20%	￥2970.00 T77865-25mg ￥2970.00 现货（买3赠1）	7 7	-	-	-	-

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产品描述：

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

靶点：

Adenosine Receptor;AdenosineReceptor

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. Cell Viability Assay Cell Line: U87MG GSCs Concentration: 10 μM Incubation Time: 72 hours Result: Decreased ~25% VEGF secretion.

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.

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.

溶解性：

Soluble in DMSO

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.476 ml	12.382 ml	24.764 ml
5 mM	0.495 ml	2.476 ml	4.953 ml
10 mM	0.248 ml	1.238 ml	2.476 ml
50 mM	0.05 ml	0.248 ml	0.495 ml

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部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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