Lercanidipine HCl
产品说明书
 |
同义名 : | 乐卡地平盐酸盐 ;Lercanidipine (hydrochloride);Lercanidipine hydrochloride |
| CAS号 : | 132866-11-6 | |
| 货号 : | A152276 | |
| 分子式 : | C36H42ClN3O6 | |
| 纯度 : | 99% | |
| 分子量 : | 648.188 | |
| MDL号 : | MFCD07773089 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
DMSO: 50 mg/mL(77.14 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
|
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Lercanidipine hydrochloride is a calcium channel blocker used in the treatment of hypertension. It is a poor water soluble drug with absolute bioavailability of 10%. However, nanostructured lipid carriers are a potential controlled release formulation for lercanidipine hydrochloride and may be a promising drug delivery system for the treatment of hypertension[3]. Lercanidipine is a lipophilic third-generation DHP-CCB (Dihydropyridine-Calcium channel blocker), characterized by high vascular selectivity and persistence in the smooth muscle cell membranes. Lercanidipine prevents renal damage induced by angiotensin II and demonstrates anti-inflammatory, antioxidant, and anti-atherogenic properties through an increasing bioavailability of endothelial nitric oxide. It is associated with a regression of microvascular structural modifications in hypertensive patients. Lercanidipine produces a sustained blood pressure-lowering activity with a high rate of responder/normalized patients, associated with a favorable tolerability profile[4]. Lercanidipine and lercanidipine/enalapril for stage 1 or 2 hypertension highly improves office SBP and DBP, overall 24-hour BP (blood pressure), daytime BP, and nighttime BP, also reducing BPV (BP variability) with few adverse effects[5]. Lercanidipine was associated with a lower risk of peripheral edema and a lower risk of treatment withdrawal because of peripheral edema than were the first-generation, but not the second-generation, dihydropyridine CCBs[6]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT00741585 | Essential Hypertension ... 展开 >> Cardiovascular Disease Stroke Chronic Kidney Disease 收起 << | Phase 4 | Completed | - | Spain ... 展开 >> CS Friol Friol, Lugo, Spain, 27220 CS Baiona Baiona, Pontevedra, Spain, 36300 CS Bueu Bueu, Pontevedra, Spain, 36930 CS A Estrada La Estrada, Pontevedra, Spain, 26680 CS A Guarda La Guardia, Pontevedra, Spain, 36780 CS Valmiñor Nigran, Pontevedra, Spain, 36250 CS Panxón Nigrán, Pontevedra, Spain, 36340 CS Tomiño Tomiño, Pontevedra, Spain, 36200 Bioengineering & Chronobilogy Labs., University of Vigo Vigo, Pontevedra, Spain, 36200 Hospital do Meixoeiro Vigo, Pontevedra, Spain, 36200 CS Calle Cuba Vigo, Pontevedra, Spain, 36202 CS A Doblada Vigo, Pontevedra, Spain, 36205 CS Coia Vigo, Pontevedra, Spain, 36209 CS Sardoma Vigo, Pontevedra, Spain, 36214 CS Teis Vigo, Pontevedra, Spain, 36216 CS Vilaboa Vilaboa, Pontevedra, Spain, 36141 CS San Roque Vilagarcía De Arousa, Pontevedra, Spain, 36600 CS Fingoi Lugo, Spain, 27002 Complexo Hospitalario Universitario de Ourense Orense, Spain, 32005 CS Lerez Pontevedra, Spain, 36156 收起 << |
| NCT01180413 | Essential Hypertension ... 展开 >> High Blood Pressure 收起 << | Phase 4 | Completed | - | Denmark ... 展开 >> Aarhus University Hospital - dept. cardiology (A) Aarhus, Denmark, 8000 收起 << |
| NCT00424801 | Microvascular Angina ... 展开 >> Hypertension 收起 << | Not Applicable | Terminated(Due to recent findi... 展开 >>ngs relating MRI contrast to nephrogenic systemic fibrosis) 收起 << | December 2008 | Denmark ... 展开 >> Aarhus Hospital Aarhus, Denmark, 8000 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
1.54mL 0.31mL 0.15mL |
7.71mL 1.54mL 0.77mL |
15.43mL 3.09mL 1.54mL |
| 参考文献 |
|---|