MRS 1220

• 产品号: M228
• CAS号: 183721-15-5
• 分子式: C21H14ClN5O2
• 分子量: 403.82116

产品别名

• 标题: MRS 1220
• IUPAC标准名: N-[9-chloro-2-(furan-2-yl)-[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-2-phenylacetamide
• IUPAC传统名: N-[9-chloro-2-(furan-2-yl)-[1,2,4]triazolo[1,5-c]quinazolin-5-yl]-2-phenylacetamide
• 别名: 9-Chloro-2-(2-furanyl)-5-((phenylacetyl)amino)-[1,2,4]triazolo[1,5-c]quinazoline

产品登记号

• MDL号: MFCD01321046
• PubChem SID: 24896720
• CAS号: 183721-15-5

产品性质

• 相关基因信息: human ... ADORA3(140)rat ... Adora1(29290), Adora2a(25369), Adora3(25370)
• 外观: white solid
• 溶解度: DMSO: soluble2 mg/mL
• 溶解度: 2-hydroxypropyl-β-cyclodextrin: insoluble
• 溶解度: H2O: insoluble
• 溶解度: ethanol: insoluble
• 个人保护装置: Eyeshields, Gloves, type N95 (US), type P1 (EN143) respirator filter
• 德国WGK号: 3

产品详细信息

详细说明 (English)

Biochem/physiol Actions
MRS1220 is a putative A3 adenosine receptor antagonist. MRS 1220 was found to be competitive in saturation binding studies using the agonist radioligand 125I AB-MECA at cloned human brain A3 receptors expressed in HEK-293 cells. Antagonism was demonstrated in functional assays consisting of agonist-induced inhibition of adenylate cyclase and the stimulation of binding of 35S guanosine 5′-O-(3-thiotriphosphate (35S GTP-gamma-S) to the associated G-proteins. MRS 1220 and MRS 1191, with KB values of 1.7 and 92 nM, respectively, proved to be highly selective for human A3 receptor vs human A1 receptor-mediated effects on adenylate cyclase. In addition, MRS 1220 reversed the effect of A3 agonist-elicited inhibition of tumor necrosis factor-alpha formation in the human macrophage U-937 cell line, with an IC50 value of 0.3 μM.