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U89232
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
U89232图片
CAS NO:134017-78-0
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
20mg电议

产品介绍
U-89232可能是一种选择性的心脏KATP通道开启剂。
Cas No.134017-78-0
Canonical SMILESCCC(C)(C)N/C(NC#N)=N\[C@H]1C2=CC(C#N)=CC=C2OC(C)(C)[C@@H]1O
分子式C19H25N5O2
分子量355.43
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

U-89232 appears to be a cardioselective KATP channel opener.

U-89232, a derivative of the ATP-sensitive potassium (KATP) channel opener Cromakalim. Experiments are performed in open-chest pigs subjected to a 60-min occlusion of the left anterior descending coronary artery (LADCA) and to 2 h of reperfusion. Four groups of animals are studied (n=6 each). Animals receive either U-89232, 3 mg/kg i.v. over a 15-min period (U), or Glibenclamide, a selective KATP channel blocker, 1 mg/kg i.v. over a 15-min period (GLI) before the LADCA occlusion. In the GLI+U group, first Glibenclamide (1 mg/kg/15 min) and then U-89232 (3 mg/kg/15 min) are infused before the 60 min of ischemia. Saline-treated animals serve as controls (CON). Hemodynamic parameters are continuously monitored. Regional contractile wall function is quantified with ultrasonic crystals aligned to measure wall thickening. At the end of the protocol, infarct size (IS, as percentage of risk region) is determined by incubating the myocardium with p-nitrobluetetrazolium. With comparable myocardium at risk, infusion of U-89232 before 60 min of LADCA occlusion significantly reduces infarct size (IS, 18.5±3.7%; p<0.001 vs. 63.2±3.3% for the controls), whereas glibenclamide has no effect on infarct size (IS, 69.5±4.4%). The administration of glibenclamide before U-89232 infusion blocks the infarct size-reducing effect of U-89232. At least in a pig model, U-89232 appears to be a cardioselective KATP channel opener, because in the absence of hemodynamic alterations, it exhibits a profound cardioprotective effect, which is fully reversible by blocking KATP channels[1].

[1]. Rohmann S, et al. In swine myocardium, the infarct size reduction induced by U-89232 is glibenclamide sensitive: evidence that U-89232 is a cardioselective opener of ATP-sensitive potassium channels. J Cardiovasc Pharmacol. 1997 Jan;29(1):69-74.