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MRS-1191
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MRS-1191图片
CAS NO:185222-90-6
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
MRS-1191 是一种有效的选择性的 A3 腺苷受体 (A3 adenosine receptor ) 拮抗剂,其 KB 值为 92 nM,对人 A3 受体的 Ki 值为 31.4 nM,对 CHO 细胞的 IC50 值为 120 nM。
Cas No.185222-90-6
Canonical SMILESO=C(OCC)C1=C(NC(C2=CC=CC=C2)=C(C1C#CC3=CC=CC=C3)C(OCC4=CC=CC=C4)=O)C
分子式C31H27NO4
分子量477.55
溶解度DMSO: 250 mg/mL (523.51 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

MRS-1191 is a potent and selective A3 adenosine receptor antagonist with a KB value of 92 nM, a Ki value of 31.4 nM for human A3 receptor and an IC50 of 120 nM for CHO cells[1].

The effects of putative A3 adenosine receptor antagonist of MRS-1191 is characterized in receptor binding and functional assays. MRS-1191 is found to be competitive in saturation binding studies using the agonist radioligand [125I]AB-MECA (N6-(4-amino-3-iodobenzyl)adenosine-5'-N-methyluronamide) at cloned human brain A3 receptor expressed in HEK-293 cells. Antagonism is 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-1191 with a KB value of 92 nM, proves to be highly selective for human A3 receptor vs human A1 receptor-mediated effects on adenylate cyclase[1].

[1]. Jacobson KA, et al. Pharmacological characterization of novel A3 adenosine receptor-selective antagonists. Neuropharmacology. 1997 Sep;36(9):1157-65.