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编 号:F662524
分子式:C22H21Cl2N3O
分子量:414.33
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10mM*1mL in DMSO
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5mg
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10mg
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25mg
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50mg
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生物活性:
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.

体内研究:
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.

体外研究:
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.
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