MRS1220_product_DataBase

Bioactivity	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].
Invitro	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]. Cell Viability Assay[2] Cell Line:
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]. Animal Model:
Name	MRS1220
CAS	183721-15-5
Formula	C21H14ClN5O2
Molar Mass	403.82
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Reference	[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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