(S)-Lercanidipine hydrochloride
(Synonyms: (S)-盐酸乐卡地平) 目录号 : GC60418
(S)-Lercanidipinehydrochloride是Lercanidipinehydrochloride的S-对映体。(S)-lercanidipinehydrochloride是一个高效的钙离子通道阻断剂。
Cas No.:184866-29-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
(S)-Lercanidipine hydrochloride is the S-enantiomer of Lercanidipine hydrochloride. (S)-lercanidipine hydrochloride is a potent calcium channel blocker[1].
[1]. Wirtz S,et al. Molecular mechanisms of vasoselectivity of the 1,4-dihydropyridine lercanidipine. Br J Pharmacol. 2004 May;142(2):275-84.
| Cas No. | 184866-29-3 | SDF | |
| 别名 | (S)-盐酸乐卡地平 | ||
| Canonical SMILES | O=C(OC(C)(CN(C)CCC(C1=CC=CC=C1)C2=CC=CC=C2)C)C3=C(NC(C)=C([C@@H]3C4=CC=CC([N+]([O-])=O)=C4)C(OC)=O)C.[H]Cl | ||
| 分子式 | C36H42ClN3O6 | 分子量 | 648.19 |
| 溶解度 | 储存条件 | Store at -20°C | |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.5428 mL | 7.7138 mL | 15.4276 mL |
| 5 mM | 0.3086 mL | 1.5428 mL | 3.0855 mL |
| 10 mM | 0.1543 mL | 0.7714 mL | 1.5428 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Lercanidipine hydrochloride versus felodipine sustained-release for mild-to-moderate hypertension: a multi-center, randomized clinical trial
Curr Med Res Opin 2015 Jan;31(1):171-6.PMID:25425015DOI:10.1185/03007995.2014.960073.
Objective: Lercanidipine hydrochloride and felodipine sustained-release tablets comparison for the treatment of patients with mild-to-moderate primary hypertension. Research design and methods: The study was designed as a multicenter, randomized, open-label, parallel-group clinical trial. A total of 281 adult patients (18-75 years) with a mild-to-moderate primary hypertension diagnosis were randomly assigned, in a 1:1 ratio, to lercanidipine hydrochloride (n = 139; 81 males) or felodipine sustained-release tablets (n = 142; 87 males). Study duration was 8 weeks, including two run-in weeks and 6 weeks of treatment. Main outcome measures: The mean seated diastolic blood pressure (BP) change from baseline to 6 weeks of treatment was the primary endpoint. Main secondary efficacy parameters were: (i) mean seated systolic BP change from baseline to 6 weeks of treatment; (ii) normalization BP rate. The incidence of adverse events was also considered. Results: BP monitoring showed a significant decrease compared with baseline in diastolic BP (lercanidipine: from 96 ± 4 to 83 ± 6 mmHg, p < 0.0001; felodipine: from 96 ± 4 to 82 ± 5 mmHg, p < 0.0001). The mean systolic BP decreased, when compared with baseline values, by 18 mmHg and 19 mmHg in the lercanidipine and felodipine arm, respectively (p < 0.0001 versus baseline for both comparisons). The normalization rates of BP were 79.5% and 87.2%, in the lercanidipine and felodipine groups, respectively (in-office monitoring; p = n.S.). In total, 73 patients experienced 103 AEs: 26.6% (37/139) in the lercanidipine group and 25.3% (36/142) in the felodipine arm (p = n.S.). The analysis of safety showed no unexpected adverse events. Conclusions: Although the overall short follow-up of the present study should be taken into account, lercanidipine is an effective and safe treatment option for BP control in adult patients with mild-to-moderate primary hypertension.
Assay of lercanidipine hydrochloride in dosage forms using nucleophilic substitution reaction
Acta Pharm 2011 Dec;61(4):457-63.PMID:22202204DOI:10.2478/v10007-011-0031-5.
A simple and sensitive spectrophotometric method has been developed for the assay of lercanidipine hydrochloride (LER) in bulk and in formulations. The method is based on the formation of coloured species between the drug and 1,2-naphthaquinone-4-sulphonic acid sodium salt (NQS) by means of nucleophilic substitution reaction. Absorbance was measured at λ(max) = 460 nm. The method was analyzed statistically. The system obeyed the Beer'S law in the range 20-100 μg mL⁻¹. Molar absorptivity value was found to be 4.79 × 10³ L mol⁻¹ cm⁻¹. Limits of detection and quantification were found to be as low as 0.04 and 0.13 μg mL⁻¹. Precision (RSD, 0.4%) and accuracy (recovery 99.2 ± 0.6 to 101.1 ± 0.8%) of the developed method were evaluated.
Combined mixture-process variable approach: a suitable statistical tool for nanovesicular systems optimization
Expert Opin Drug Deliv 2016 Jun;13(6):777-88.PMID:27020331DOI:10.1517/17425247.2016.1166202.
Objectives: This study aims to illustrate the applicability of combined mixture-process variable (MPV) design and modeling for optimization of nanovesicular systems. Methods: The D-optimal experimental plan studied the influence of three mixture components (MCs) and two process variables (PVs) on lercanidipine transfersomes. The MCs were phosphatidylcholine (A), sodium glycocholate (B) and lercanidipine hydrochloride (C), while the PVs were glycerol amount in the hydration mixture (D) and sonication time (E). The studied responses were Y1: particle size, Y2: zeta potential and Y3: entrapment efficiency percent (EE%). Polynomial equations were used to study the influence of MCs and PVs on each response. Response surface methodology and multiple response optimization were applied to optimize the formulation with the goals of minimizing Y1 and maximizing Y2 and Y3. Results: The obtained polynomial models had prediction R(2) values of 0.645, 0.947 and 0.795 for Y1, Y2 and Y3, respectively. Contour, Piepel'S response trace, perturbation, and interaction plots were drawn for responses representation. The optimized formulation, A: 265 mg, B: 10 mg, C: 40 mg, D: zero g and E: 120 S, had desirability of 0.9526. The actual response values for the optimized formulation were within the two-sided 95% prediction intervals and were close to the predicted values with maximum percent deviation of 6.2%. Conclusions: This indicates the validity of combined MPV design and modeling for optimization of transfersomal formulations as an example of nanovesicular systems.