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LUF6000
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。
LUF6000图片
CAS NO:890087-21-5
包装与价格：
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
LUF6000 是一种具有口服活性的 A3 腺苷受体变构调节剂。
Cas No.890087-21-5
别名N-(3,4-二氯苯基)-2-环己基-1H-咪唑并[4,5-C]喹啉-4-胺,LUF-6000;LUF 6000
化学名2-cyclohexyl-N-(3,4-dichlorophenyl)-3H-imidazo[4,5-c]quinolin-4-amine
Canonical SMILESC1CCC(CC1)C2=NC3=C(N2)C(=NC4=CC=CC=C43)NC5=CC(=C(C=C5)Cl)Cl
分子式C22H20Cl2N4
分子量411.33
溶解度Soluble in DMSO
储存条件Store at -20℃
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

LUF6000 is an allosteric modulator of the human A3 adenosine receptor (AR). IC50 value: Target: A3 adenosine receptor LUF6000 was found to be an allosteric enhancer of Emax of structurally diverse agonists at the A3 AR, being more effective for low-Emax agonists than for high-Emax agonists. LUF6000 exerted an Emax-enhancing effect at a concentration of 0.1 microM or higher, and was shown to increase the Emax of Cl-IB-MECA and other low-efficacy agonists to a larger extent than that of the high-efficacy agonist NECA. Interestingly, LUF6000 converted a nucleoside A3 AR antagonist MRS542, but not a non-nucleoside antagonist MRS1220, into an agonist.

References:
[1]. Gao ZG, Verzijl D, Zweemer A et al. Functionally biased modulation of A(3) adenosine receptor agonist efficacy and potency by imidazoquinolinamine allosteric enhancers. Biochem Pharmacol. 2011 Sep 15;82(6):658-68. doi: 10.1016/j.bcp.2011.06.017.
[2]. Szentmiklósi AJ, Cseppento A, Harmati G, Nánási PP. Novel trends in the treatment of cardiovascular disorders: site- and event- selective adenosinergic drugs. Curr Med Chem. 2011;18(8):1164-87.
[3]. Heitman LH, G bly s A, Zweemer AM, et al. A series of 2,4-disubstituted quinolines as a new class of allosteric enhancers of the adenosine A3 receptor. J Med Chem. 2009 Feb 26;52(4):926-31.
[4]. Gao ZG, Ye K, G bly s A, et al. Flexible modulation of agonist efficacy at the human A3 adenosine receptor by the imidazoquinoline allosteric enhancer LUF6000. BMC Pharmacol. 2008 Dec 12;8:20.
[5]. G bly s A, Gao ZG, Brussee J, et al. Structure-activity relationships of new 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric enhancers of the A3 adenosine receptor. J Med Chem. 2006 Jun 1;49(11):3354-61.