LUF6096

LUF6096

L655767-1ml

1ml

10mM in DMSO

-80℃储存

超低温冰袋运输

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 In Vitro LUF6096 (10 μM; 30-120 min) decreases the dissociation rate of 125 I-AB-MECA from the A 3 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. IC50& Target:adenosine A3 receptor

LUF6096 是腺苷 A3 受体的一种强效异构增强剂，能够异构增强激动剂的结合。LUF6096 对任何腺苷受体都显示出较低的正交亲和力。LUF6096 对心肌缺血/再缺血具有保护作用。

1116652-18-6(DMSO)

C22H21Cl2N3O

414.33 g/mol

C1CCC(CC1)C(=O)NC2=CC(=NC3=CC=CC=C32)NC4=CC(=C(C=C4)Cl)Cl