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LUF6000

Catalog No. T15791 CAS 890087-21-5

LUF6000 is an allosteric modulator of the human A3 adenosine receptor (AR).

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LUF6000, CAS 890087-21-5

Pack Size	Availability	Price/USD
5 mg	6-8 weeks	$ 327.00
25 mg	6-8 weeks	$ 767.00
50 mg	6-8 weeks	$ 997.00
100 mg	6-8 weeks	$ 1,750.00
1 mL * 10 mM (in DMSO)	6-8 weeks	$ 358.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

Storage & Solubility Information

Description

LUF6000 is an allosteric modulator of the human A3 adenosine receptor (AR).

In vitro

LUF6000 converted a nucleoside A3 AR antagonist MRS542, but not a non-nucleoside antagonist MRS1220, into an agonist. 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. 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.

Molecular Weight	411.33
Formula	C22H20Cl2N4
CAS No.	890087-21-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 14.29 mg/mL (34.74 mM), Sonication is recommended.

References and Literature

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. Göblyös 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.

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

LUF6000 890087-21-5 Others LUF-6000 LUF 6000 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.