1116652-18-6

1116652-18-6 structure

Name: LUF6096
Chemical Name: N-[2-(3,4-dichloroanilino)quinolin-4-yl]cyclohexanecarboxamide
CAS Number: 1116652-18-6
Molecular Formula: C₂₂H₂₁Cl₂N₃O
Molecular Weight: 414.32800
Catalog: Signaling Pathways GPCR/G Protein Adenosine Receptor
Create Date: 2017-09-23 08:54:41
Modify Date: 2024-01-16 14:44:12
LUF6096, a potent allosteric enhancer of the adenosine A3 receptor, is able to allosterically enhance agonist binding. LUF6096 shows low orthosteric affinity for any of the adenosine receptors. LUF6096 shows protective effects in myocardial ischemia/reperfusion injury[1][2].

Name	N-[2-(3,4-dichloroanilino)quinolin-4-yl]cyclohexanecarboxamide
Synonyms	unii-qxa2220n3t luf-6096 cf-602

Description	LUF6096, a potent allosteric enhancer of the adenosine A3 receptor, is able to allosterically enhance agonist binding. LUF6096 shows low orthosteric affinity for any of the adenosine receptors. LUF6096 shows protective effects in myocardial ischemia/reperfusion injury[1][2].
Related Catalog	Research Areas >> Cardiovascular Disease Signaling Pathways >> GPCR/G Protein >> Adenosine Receptor
Target	adenosine A3 receptor[1]
In Vitro	LUF6096 (10 μM; 30-120 min) decreases the dissociation rate of 125I-AB-MECA from the A3 receptor by 2.5 times in CHO cell membranes[1]. LUF6096 (10 μM; pretreated for 15 min) significantly and dramatically enhances the intrinsic activity of Cl-IB-MECA for the inhibition of the forskolin-stimulated cAMP production in CHO cells[1].
In Vivo	LUF6096 (twice i.v. bolus for 0.5 mg/kg or single i.v. bolus for 1 mg/kg) protects against myocardial ischemia/reperfusion injury in dogs[1]. Animal Model: Adult mongrel dogs (15-25 kg) were subjected left anterior descending (LAD) coronary artery occlusion and reperfusion[1] Dosage: Twice i.v. bolus for 0.5 mg/kg or single i.v. bolus for 1 mg/kg Administration: I.v. bolus Result: Produced a marked reduction in infarct size (∼50% reduction) compared with vehicle-treated dogs.
References	[1]. Heitman LH, 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. [2]. Du L, et, al. Protection from myocardial ischemia/reperfusion injury by a positive allosteric modulator of the A₃ adenosine receptor. J Pharmacol Exp Ther. 2012 Jan;340(1):210-7.

Molecular Formula	C₂₂H₂₁Cl₂N₃O
Molecular Weight	414.32800
Exact Mass	413.10600
PSA	60.74000
LogP	6.87540
Storage condition	-20°C

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