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MRS 1220_分子结构_CAS_183721-15-5)
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MRS 1220

产品号 M228 公司名称 Sigma Aldrich
CAS号 183721-15-5 公司网站 http://www.sigmaaldrich.com
分子式 C21H14ClN5O2 电 话 1-800-521-8956
分子量 403.82116 传 真
纯 度 电子邮件
保 存 Chembase数据库ID: 132285

产品价格信息

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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.

参考文献