Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Nicorandil (SG-75) 是一种有效的钾通道激活剂,靶向血管核苷二磷酸依赖性 K+通道和心脏 ATP 敏感 K+通道 (KATP)。Nicorandil 是一种烟酰胺酯,具有血管舒张和心脏保护作用,并具有治疗心绞痛和缺血性心脏病的潜力。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
50 mg | ¥ 327 | 现货 | ||
100 mg | ¥ 460 | 现货 | ||
500 mg | ¥ 1,110 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 510 | 现货 |
产品描述 | Nicorandil (SG-75)(Ikorel) acts by relaxing the smooth muscle of the blood vessels, especially those of the venous system. It undertakes this through two methods. Firstly, by activating potassium channels, and secondly by donating nitric oxide to activate the enzyme guanylate cyclase. Guanylate cyclase causes activation of cGMP leading to both arterial and venous vasodilatation by de-phosphorylation of the myosin light chain. |
体外活性 | Nicorandil (100 mM) increases Flavoprotein oxidation but not membrane current; a 10-fold higher concentration recruits both mitoK(ATP) and surfaceK(ATP) channels. Nicorandil bluntes the rate of cell death in a pelleting model of ischemia; this cardioprotective effect is prevented by the mitoK(ATP) channel blocker 5-hydroxydecanoate but is unaffected by the surfaceK(ATP) channel blocker HMR1098. [1] Nicorandil (100 mM) suppresses TUNEL positivity, cytochrome c translocation, caspase-3 activation and dissipation of mitochondrialinner membrane potential (Delta(Psi)(m)). Nicorandil prevents Delta(Psi)(m) depolarization in a concentration-dependent manner (EC(50) approximately 40 mM, with saturation by 100 mM), as shown by fluorescence-activated cell sorter analysis of cells stained with a fluorescent Delta(Psi)(m)-indicator, tetramethylrhodamine ethyl ester (TMRE). [2] Nicorandil activates a weakly inwardly-rectifying, glibenclamide-sensitive 80 pS K+ channel in both the transfected cells. Nicorandil preferentially activates the K(ATP) channels containing SUR2B in HEK293T cells. [3] Nicorandil (100 mM) significantly suppresses the number of cells with TUNEL-positive nuclei and the increase in caspase-3 activity induced by 20 mM Water2. Nicorandil prevents the loss of DeltaPsim induced by Water2 in a concentration-dependent manner. [4] |
别名 | SG-75, 尼可地尔 |
分子量 | 211.17 |
分子式 | C8H9N3O4 |
CAS No. | 65141-46-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 80.5 mM
DMSO: 198.9 mM
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
H2O / DMSO | 1 mM | 4.7355 mL | 23.6776 mL | 47.3552 mL | 118.388 mL |
5 mM | 0.9471 mL | 4.7355 mL | 9.471 mL | 23.6776 mL | |
10 mM | 0.4736 mL | 2.3678 mL | 4.7355 mL | 11.8388 mL | |
20 mM | 0.2368 mL | 1.1839 mL | 2.3678 mL | 5.9194 mL | |
50 mM | 0.0947 mL | 0.4736 mL | 0.9471 mL | 2.3678 mL | |
DMSO | 100 mM | 0.0474 mL | 0.2368 mL | 0.4736 mL | 1.1839 mL |
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。
Nicorandil 65141-46-0 Membrane transporter/Ion channel Potassium Channel angina SG-75 diphosphate-dependent channels diseases cardioprotective inhibit KATP 尼可地尔 KcsA nucleoside Inhibitor SG75 vascular vasodilatory SG 75 ATP forischemic heart inhibitor