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KRN4884  

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包装规格：100mg in glass bottle
产品描述：基本信息 产品编号： K10134  产品名称： KRN4884 CAS: 152802-84-1   储存条件 粉末 -20℃ 四年 分子式： C15H14ClN5 溶于液体 -80℃ 一年 分子量： 299.76     化学名：  5-amino-N-cyano-N'-[2-(2-chlorophenyl)ethyl]-3-pyridinecarboximidamide 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K+通道开放剂。在细胞内ATP(1mM)存在下，KRN4884(0.1-3μM)激活KATP通道(EC50=0.55μM),这种作用存在浓度依赖性。 靶点 EC50:0.55μM (KATP channel)   体外研究 KRN4884 (0.3μM) shifts the concentration-response relationship for ATP-induced KATP channel inhibition to the right and slightly upward direction without altering the slope.After either the spontaneous or Ca2+-induced channel rundown,KRN4884 (1 and 3μM) partially restores the KATP channel activity.Furthermore, the effect of KRN4884 is augmented by the presence of uridine 5′-diphosphate (3mM).KRN4884 activates cardiac KATP channels through not only decreasing the sensitivity of the channel to ATP but also directly stimulating the opening of the channel.KRN4884 (0.3 and 3μM) increases the outward current in a concentration-dependent manner,and the unitary current amplitudes are similar to that of KATP channels in the ATP-free solution. 体内研究 The effects of KRN4884,a novel pyridinecarboxamidine type KATP channel opener,on serum triglyceride levels are investigated in Sprague-Dawley rats.Oral administration of KRN4884 (3mg/kg) for 10 days causes a significant reduction in serum triglyceride levels, which is comparable to that of Clofibrate (160mg/kg).Reduction in serum triglyceride levels by KRN4884 and Clofibrate are accompanied by a reduction in triglyceride levels both in chylomicron and in very low density lipoprotein.KRN4884 treatment does not affect serum concentrations of total cholesterol and phospholipid,but increases free fatty acid levels.Rats receiving KRN4884 exhibite an increase in lipoprotein lipase (LPL) activity both in adipose tissue and in skeletal muscle.   推荐实验方法(仅供参考) 激酶实验： KRN4884 is dissolved in DMSO as a 10mM stock solution,and diluted in the bath solution.The final concentration of DMSO to which cells are exposed is less than 0.1%.To quantitatively analyze the effect of KRN4884 or other compounds, channel activity is expressed as NPoi.NPoi is calculated by integrating a 5- to 15-s continuous current record during the steady effect of each drug.The concentrationresponse curve for KRN4884 is obtained by normalizing NPoi to that obtained by superfusing with the ATP-free bath solution,and fit to a Hill equation.   动物实验:   Rats Five-week old male Sprague-Dawley (Crj;CD) rats are obtained and housed in a temperature-controlled environment with a 12h daily light cycle with free access to water and chow (CE-2).At 6-weeks old,the animals are assigned to vehicle,Clofibrate (160mg/kg) or KRN4884 (3mg/kg) treatment groups.The drug is given daily,by gavage for 10 days at 2mL/kg as a suspension in 0.5% (w/v) carboxymethyl cellulose.Systolic blood pressure is determined 1h after administration on day 9 with the tail cu.method by use of a sphygmomanometer.Four hours after the final administration of the drug or vehicle on day 10,non-fasting blood is collected from an abdominal aorta of each rat under ether anaesthesia.Serum is provided for lipid analysis.Epididymal adipose tissue,thigh muscle,and liver are removed and weighed,then immediately immersed in liquid nitrogen and stored at -80℃ until use.Epididymal adipose tissue and thigh muscle are used for determining lipoprotein lipase (LPL) activity and the liver is used for de- termining hepatic triglyceride lipase (HTGL) activity.
保存条件：-20℃

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