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LUF6000 Inhibitor

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5755122

MBS5755122 is an inhibitor targeting LUF6000. LUF6000 is an allosteric modulator of the human A3 adenosine receptor (AR). More details

Product Documentation
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Sample Manual Insert View PDF
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Testing Data View PDF
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Certificate of Analysis (COA) View PDF
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QC Report View PDF
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Material Safety Data Sheet View PDF
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Technical Datasheet View PDF
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Protocol View PDF

Product Overview

Online Datasheet in PDF
Product Name
LUF6000, Inhibitor
Full Product Name
LUF6000
Product Gene Name
Form/Format
Solid. Powder
Purity/Purification
98.00%
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
Molecular Weight
411.33
Solubility
DMSO: 14.29mg/mL (34.74mM) Need ultrasonic
(<1mg/ml refers to the product slightly soluble or insoluble)
Formula
C22H20Cl2N4
SMILES
ClC1=CC(NC2=NC3=C(C=CC=C3)C4=C2NC(C5CCCCC5)=N4)=CC=C1Cl
CAS Number
890087-21-5
Target & IC50
Others
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 0.1microM 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.

Structure of LUF6000, inhibitor

LUF6000 Inhibitor – Cat# MBS5755122

Product References and Citations for LUF6000, inhibitor

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.
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.
Szentmiklosi AJ, Cseppento A, Harmati G, Nanasi PP. Novel trends in the treatment,of cardiovascular disorders: site- and event- selective adenosinergic drugs. Curr Med Chem. 2011;18(8):1164-87.
Szentmiklosi AJ, Cseppento A, Harmati G, Nanasi PP. Novel trends in the treatment,of cardiovascular disorders: site- and event- selective adenosinergic drugs. Curr Med Chem. 2011;18(8):1164-87.
Heitman LH, Goblyos 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.
Heitman LH, Goblyos 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.
Gao ZG, Ye K, Goblyos 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.
Gao ZG, Ye K, Goblyos 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.
Goblyos 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.
Goblyos 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.

Other Notes

Small volumes of LUF6000, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.
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