Powder: -20°C for 3 years | In solvent: -80°C for 1 year
KRN 4884 is an opener of the K+ channel. KRN 4884 (0.1-3 μM) activates KATP channels in a concentration-dependent manner (EC50=0.55 μM), in the presence of intracellular ATP (1 mM).
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 10,600 | 6-8周 | ||
50 mg | ¥ 13,800 | 6-8周 | ||
100 mg | ¥ 17,500 | 6-8周 |
产品描述 | KRN 4884 is an opener of the K+ channel. KRN 4884 (0.1-3 μM) activates KATP channels in a concentration-dependent manner (EC50=0.55 μM), in the presence of intracellular ATP (1 mM). |
靶点活性 | KATP channel:(EC50)0.55 μM |
体外活性 | KRN4884 (1 and 3 μM) partially restores the KATP channel activity, after either the spontaneous or Ca2+-induced channel rundown. 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 3 μM) 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. KRN4884 (0.3 μM) shifts the concentration-response relationship for ATP-induced KATP channel inhibition to the right and slightly upward direction without altering the slope. The effect of KRN4884 is augmented by the presence of uridine 5′-diphosphate (3 mM) [1]. |
体内活性 | 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. KRN4884 (3 mg/kg; p.o.; 10 days) treatment, leads to a significant reduction in serum triglyceride levels, which is comparable to that of Clofibrate (160 mg/kg). The effects of KRN4884, a novel pyridinecarboxamidine type KATP channel opener, on serum triglyceride levels are investigated in Sprague-Dawley rats. 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 [2]. |
分子量 | 299.76 |
分子式 | C15H14ClN5 |
CAS No. | 152802-84-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
KRN4884 152802-84-1 Others KRN 4884 KRN-4884 Inhibitor inhibitor inhibit