U89232
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| 包装规格: | 100mg in glass bottle |
| 产品描述: | 基本信息 产品编号: U10114 产品名称: U89232 CAS: 134017-78-0 储存条件 粉末 -20℃ 四年 分子式: C19H25N5O2 溶于液体 -80℃ 一年 分子量: 355.43 化学名: 1-cyano-2-[(3R,4S)-6-cyano-3-hydroxy-2,2-dimethyl-3,4-dihydrochromen-4-yl]-3-(2-methylbutan-2-yl)guanidine Solubility (25°C): 体外: DMSO Ethanol Water 体内(现配现用): <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 生物活性 产品描述 一种选择性的心脏KATP通道开启剂。 靶点 KATP channel 体内研究 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 2h of reperfusion.Four groups of animals are studied (n=6 each).Animals receive either U-89232,3mg/kg i.v.over a 15-min period (U),or Glibenclamide,a selective KATP channel blocker,1mg/kg i.v.over a 15-min period (GLI) before the LADCA occlusion.In the GLI+U group,first Glibenclamide (1mg/kg/15 min) and then U 89232 (3mg/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. |
| 保存条件: | -20℃ |
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