MRS 1220

产品名称：

183721-15-5
MRS 1220
9-Chloro-2-(2-furanyl)-5-((phenylacetyl)amino)-[1,2,4]triazolo[1,5-c]quinazoline

产品介绍：

产品说明

包装

5, 25 mg in glass bottle

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.

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.

基本信息

经验(实验)分子式	C₂₁H₁₄ClN₅O₂
分子量	403.82
MDL编号	MFCD01321046
PubChem化学物质编号	24896720
NACRES	NA.77

产品性质

质量水平	100
形式	solid
颜色	white
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)

安全信息

储存分类代码	11 - Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable
个人防护装备	Eyeshields, Gloves, type N95 (US)