LUF6096

Research use only, not for human use.

LUF6096 (CF-602) is a potent allosteric enhancer of the adenosine A3 receptor, exhibiting the capability to enhance agonist binding allosterically while demonstrating low orthosteric affinity across adenosine receptors.

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.

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.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..

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.Animal Model:Adult mongrel dogs (15-25 kg) were subjected left anterior descending (LAD) coronary artery occlusion and reperfusion 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.

——

GPCR/G Protein

Adenosine Receptor

Adenosine Receptor

——

——

1116652-18-6

414.33

C22H21Cl2N3O

>98% (HPLC)

In Vitro:?DMSO : 20 mg/mL (48.27 mM; Ultrasonic (<60°C)

Clc1ccc(Nc2cc(NC(=O)C3CCCCC3)c3ccccc3n2)cc1Cl

——

(-20℃)

With Ice Pack

≥ 2 years