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MRS 1220
产品别名
183721-15-5
MRS 1220
9-Chloro-2-(2-furanyl)-5-((phenylacetyl)amino)-[1,2,4]triazolo[1,5-c]quinazoline
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C21H14ClN5O2 |
| Molecular weight | 403.82 |
| MDL number | MFCD01321046 |
| PubChem Substance ID【PubChem化学物质编号】 | 24896720 |
| NACRES | NA.77 |
| Biochem/physiol Actions【生化/生理作用】 | 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. |
| Features and Benefits【特点和优势】 | This compound is featured on the Adenosine Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here. |
产品性质
| Quality Level【质量水平】 | 100 |
| form【形式】 | solid |
| color【颜色】 | white |
| solubility【溶解性】 | DMSO: 2 mg/mL 2-hydroxypropyl-β-cyclodextrin: insoluble H2O: insoluble ethanol: insoluble |
| SMILES string | Clc1ccc2nc(NC(=O)Cc3ccccc3)n4nc(nc4c2c1)-c5ccco5 |
| InChI | 1S/C21H14ClN5O2/c22-14-8-9-16-15(12-14)20-25-19(17-7-4-10-29-17)26-27(20)21(23-16)24-18(28)11-13-5-2-1-3-6-13/h1-10,12H,11H2,(H,23,24,28) |
| InChI key | TWWFAXQOKNBUCR-UHFFFAOYSA-N |
| Gene Information | human ... ADORA3(140) rat ... Adora1(29290), Adora2a(25369), Adora3(25370) |
| packaging【包装】 | 5, 25 mg in glass bottle |
安全信息
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 3 |
| Personal Protective Equipment【个人防护装备】 | Eyeshields, Gloves, type N95 (US) |
