890087-21-5

890087-21-5 structure

Name: LUF6000
Chemical Name: 2-cyclohexyl-N-(3,4-dichlorophenyl)-3H-imidazo[4,5-c]quinolin-4-amine
CAS Number: 890087-21-5
Molecular Formula: C₂₂H₂₀Cl₂N₄
Molecular Weight: 411.32700
Catalog: Signaling Pathways GPCR/G Protein Adenosine Receptor
Create Date: 2017-04-20 03:42:34
Modify Date: 2024-01-02 18:04:27
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.

Name	2-cyclohexyl-N-(3,4-dichlorophenyl)-3H-imidazo[4,5-c]quinolin-4-amine
Synonyms	luf6000\|\|luf 6000 cs-1158 luf6000

Description	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.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Adenosine Receptor Research Areas >> Cardiovascular Disease
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.

Molecular Formula	C₂₂H₂₀Cl₂N₄
Molecular Weight	411.32700
Exact Mass	410.10700
PSA	56.83000
LogP	6.63110
Storage condition	2-8℃

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