Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Lercanidipine hydrochloride (Corifeo) 是亲脂性二氢吡啶-钙通道阻滞剂,具有持久的降压作用和保护肾脏作用。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
10 mg | ¥ 444 | 现货 | ||
50 mg | ¥ 1,655 | 现货 | ||
100 mg | ¥ 2,390 | 现货 | ||
200 mg | ¥ 3,271 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 397 | 现货 |
产品描述 | Lercanidipine hydrochloride (Corifeo) is a calcium channel blocker of the dihydropyridine class. |
体外活性 | In vitro calcium antagonistic activity of Lercanidipine is clearly related to a gradual block of calcium entry into smooth muscle cells via L-type calcium channels. lercanidipine inhibits cellular cholesteryl ester formation. At concentrations similar to those occurring in clinical practice, it may inhibit in vitro macrophage functions involved in atherogenesis and plaque stability[1]. |
体内活性 | In chronically catheterised dogs with experimental renovascular hypertension, lercanidipine decreases diastolic blood pressure in a dose-dependent manner (ED25 = 0.9 mg/kg p.o). In the same animals, long term application of lercanidipine showed permanent decrease of diastolic blood pressure indicating no tolerance of the antihypertensive effect[3]. Lercanidipine possesses significant anticonvulsant effect. It does not affect the muscle coordination or locomotor activity in mice[5]. In clinical studies, lercanidipine has a 24-hour antihypertensive effect and causes no significant increase in heart rate. Lercanidipine has been shown to be effective in a wide range of hypertensive patients, including mild-to-moderate hypertension, severe hypertension, the elderly, and those with isolated systolic hypertension. It is associated with a low rate of adverse events[4]. |
激酶实验 | Cell-free enzyme assays are performed to determine the selective inhibition of ROCK1 and ROCK2 by SLx-2119. Reactions are performed on non-binding surface microplates. Four mU of human ROCK1 and ROCK2 are used to phosphorylate 30 μM of the synthetic ROCK peptide substrate S6 Long, prepared at American Peptide with the addition of 10 μM ATP, containing?33P-ATP in the presence of 10 mM Mg2+, 50 mM Tris, pH 7.5, 0.1 mM EGTA and 1 mM DTT at room temperature. One unit is the amount of kinase needed to catalyze the transfer of 1 nmol phosphate/min to the peptide. The reactions are allowed to proceed for 45 minutes and then stopped with 3% phosphoric acid to a final concentration of 1%. The reactions are captured on phospho cellulose filtration microplates and washed with 75 mM phosphoric acid and methanol using a vacuum manifold. Phosphorylation is measured on a Perkin-Elmer MicroBeta 1450. |
细胞实验 | Cells are incubated for 24 hours in DMEM+EFAF 0.2% and lercanidipine, then with lercanidipine and AcLDL for 24 hours. In the last 2 hours [14C]-oleic acid albumin complex is added for the determination of cholesterol esterification (ACAT activity). (Only for Reference) |
别名 | Corifeo, Carmen, Cardiovasc, 乐卡地平盐酸盐, 盐酸乐卡地平 |
分子量 | 648.19 |
分子式 | C36H41N3O6·HCl |
CAS No. | 132866-11-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 64.8 mg/mL (100 mM)
Ethanol: 6.5 mg/mL (10 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 1.5428 mL | 7.7138 mL | 15.4276 mL | 38.5689 mL |
5 mM | 0.3086 mL | 1.5428 mL | 3.0855 mL | 7.7138 mL | |
10 mM | 0.1543 mL | 0.7714 mL | 1.5428 mL | 3.8569 mL | |
DMSO | 20 mM | 0.0771 mL | 0.3857 mL | 0.7714 mL | 1.9284 mL |
50 mM | 0.0309 mL | 0.1543 mL | 0.3086 mL | 0.7714 mL | |
100 mM | 0.0154 mL | 0.0771 mL | 0.1543 mL | 0.3857 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。
Lercanidipine hydrochloride 132866-11-6 Membrane transporter/Ion channel Metabolism Calcium Channel Corifeo antihypertensive Inhibitor calcium Lercanidipine Lercanidipine Hydrochloride Carmen reno-protective Ca2+ channels Cardiovasc Ca channels channel 乐卡地平盐酸盐 inhibit 盐酸乐卡地平 inhibitor