Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Nisoldipine (BAY-k 5552) 是一种高效特异的L 型Cav1.2通道阻断剂,IC50=10 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
50 mg | ¥ 327 | 现货 | ||
100 mg | ¥ 460 | 现货 | ||
500 mg | ¥ 798 | 现货 | ||
1 g | ¥ 1,347 | 现货 |
产品描述 | Nisoldipine (BAY-k 5552) is a dihydropyridine calcium channel antagonist that acts as a potent arterial vasodilator and antihypertensive agent. |
靶点活性 | Cav 1.2, L-type:10 nM |
体外活性 | 对于Timothy综合征病人,Nisoldipine(IC50=267 nM)通过抑制钙离子从L型钙通道流入,降低动脉平滑肌收缩性及随后的血管收缩 , 导致血管舒张,且降低血压. |
体内活性 | 在豚鼠心室肌细胞中,Nisoldipine延迟整流K+通道,快速激活延迟整流K+通道抑制IKr(IC50=23 μM), 及缓慢激活延迟整流K+通道抑制IKs(IC50=40 μM)。 |
激酶实验 | Binding experiments of electrophysiology: CHO cells expressing the subunit of the voltage-dependent L-type Ca2+ channel are cultrured in medium without serum in the presence of different concentrations of Nisoldipine. Then Ca2+ channel current elicited from a holding potential of -100 mV or -50 mV is recorded at room temperature with the whole-cell configuration of the patch-clamp method using the List EPC-7 patch-clamp amplifer and pClamp software. The concentration of competitor inhibiting 50% of the specific binding represents IC50. |
细胞实验 | The myocytes are bathed in normal Tyrode's solution, held at -80 mV, and depolarised after 200-ms prepulses (-40mV) to more positive potentials for 500 ms at 0.1 Hz, tail currents are recorded on repolarisations to -40mV. The myocytes are exposed to 10-100 mM Nisoldipine for 8-10 minutes. Then the whole-cell membrane currents are recorded using an EPC-7 amplifier.(Only for Reference) |
别名 | 尼索地平, BAY-k 5552 |
分子量 | 388.41 |
分子式 | C20H24N2O6 |
CAS No. | 63675-72-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 56 mg/mL (144.2 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 71 mg/mL (182.8 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.5746 mL | 12.873 mL | 25.746 mL | 64.365 mL |
5 mM | 0.5149 mL | 2.5746 mL | 5.1492 mL | 12.873 mL | |
10 mM | 0.2575 mL | 1.2873 mL | 2.5746 mL | 6.4365 mL | |
20 mM | 0.1287 mL | 0.6436 mL | 1.2873 mL | 3.2182 mL | |
50 mM | 0.0515 mL | 0.2575 mL | 0.5149 mL | 1.2873 mL | |
100 mM | 0.0257 mL | 0.1287 mL | 0.2575 mL | 0.6436 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。
Nisoldipine 63675-72-9 Immunology/Inflammation Membrane transporter/Ion channel Metabolism NF-Κb Calcium Channel Reactive Oxygen Species Ca2+ channels Inhibitor inhibit 尼索地平 Ca channels BAY-k 5552 inhibitor