Levamlodipine besylate
(Synonyms: 苯磺酸左旋氨氯地平,(S)-Amlodipine besylate; Levoamlodipine besylate) 目录号 : GC34912
Levamlodipine Besylate is a powerful dihydropyridine calcium channel blocker, possessing vasodilation properties and used in the treatment of hypertension and angina.
Cas No.:150566-71-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Levamlodipine Besylate is a powerful dihydropyridine calcium channel blocker, possessing vasodilation properties and used in the treatment of hypertension and angina.
[1] Jain R, et al. Mater Sci Eng C Mater Biol Appl. 2016 Aug 1;65:205-14.
| Cas No. | 150566-71-5 | SDF | |
| 别名 | 苯磺酸左旋氨氯地平,(S)-Amlodipine besylate; Levoamlodipine besylate | ||
| Canonical SMILES | O=C(C1=C(COCCN)NC(C)=C(C(OC)=O)[C@@H]1C2=CC=CC=C2Cl)OCC.OS(C3=CC=CC=C3)(=O)=O | ||
| 分子式 | C26H31ClN2O8S | 分子量 | 567.05 |
| 溶解度 | DMSO : ≥ 150 mg/mL (264.53 mM) | 储存条件 | -20°C, protect from light |
| 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 | 1.7635 mL | 8.8176 mL | 17.6351 mL |
| 5 mM | 0.3527 mL | 1.7635 mL | 3.527 mL |
| 10 mM | 0.1764 mL | 0.8818 mL | 1.7635 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。
Effect of low-dose Levamlodipine besylate in the treatment of vascular dementia
Sci Rep 2019 Dec 3;9(1):18248.PMID:31796756DOI:10.1038/s41598-019-47868-0.
Vascular dementia (VaD) is a complex disorder caused by reduced blood flow in the brain. However, there is no effective pharmacological treatment option available until now. Here, we reported that low-dose Levamlodipine besylate could reverse the cognitive impairment in VaD mice model of right unilateral common carotid arteries occlusion (rUCCAO). Oral administration of Levamlodipine besylate (0.1 mg/kg) could reduce the latency to find the hidden platform in the MWM test as compared to the vehicle group. Furthermore, vehicle-treated mice revealed reduced phospho-CaMKII (Thr286) levels in the hippocampus, which can be partially restored by Levamlodipine besylate (0.1 mg/kg and 0.5 mg/kg) treatment. No significant outcome on microglia and astrocytes were observed following Levamlodipine besylate treatment. This data reveal novel findings of the therapeutic potential of low-dose Levamlodipine besylate that could considerably enhance the cognitive function in VaD mice.
Clinical assessment of Levamlodipine besylate combination therapy for essential hypertension: A protocol for systematic review and meta-analysis
Medicine (Baltimore) 2022 Apr 1;101(13):e29148.PMID:35421067DOI:10.1097/MD.0000000000029148.
Background: Essential hypertension has been regarded a significant risk factor for cardiovascular disease across the globe, and a significant escapable causation of early death as well as morbidity in the U.S. When angiotensin II receptor blockers and calcium channel blockers are used to treat essential hypertension, most patients will have inadequate blood pressure management. As a result, including a diuretic in the regimen is necessary. The current study's aim is to investigate the effectiveness as well as safety of Levamlodipine besylate combination therapy in treating essential hypertension at varying degrees of severity. Methods: In establishing the effectiveness and safety of the mix of Levamlodipine besylate and dihydropyridine for essential hypertension, the authors will conduct a systematic review and, where applicable, a meta-analysis of randomized controlled clinical trials. A total of 8 electronic databases will be used in the search, including 4 English databases (PubMed, Web of Science, EMBASE, and Cochrane Library) and 4 Chinese databases (China National Knowledge Infrastructure, Chinese BioMedical Literature database, Chinese Scientific Journal database, and WanFang database). All articles published in the databases will be considered between their inception and January 18, 2022. Only articles published in English or Mandarin Chinese will be picked. A group of writers will independently evaluate each reference to see if it is eligible and whether there are any duplicates. The same authors will do data extraction for all eligible studies and use the Cochrane risk of bias tool to evaluate the risk of bias in the trials chosen for inclusion. Results: The analysis will evaluate the efficiency and level of safeness of Levamlodipine besylate combined treatment for essential hypertension. Conclusions: Our systematic review will offer evidence for judging whether Levamlodipine besylate combination therapy can be considered an effective intercession for essential hypertension. Ethics and dissemination: Ethical approval will not be required as no original data will be collected as part of this review. Registration number: DOI 10.17605/OSF.IO/H8ZR2.
Bioequivalence of Levamlodipine besylate tablets in healthy Chinese subjects: a single-dose and two-period crossover randomized study
BMC Pharmacol Toxicol 2020 Nov 19;21(1):80.PMID:33213527DOI:10.1186/s40360-020-00459-6.
Background: Levamlodipine, a calcium channel blocker, has been show act as a cardiovascular drug. To compare the pharmacokinetic parameters between levamlodipine (test formulation) at a single dose of 5 mg and amlodipine (reference formulation) at a single dose of 10 mg, the bioequivalence study was carried out. Methods: A single-dose randomized, open-label, two-period crossover study was designed in healthy Chinese subjects. 48 subjects were divided into fasted and fed groups equally. The subjects randomly received the test or reference formulations at the rate of 1:1. Following a 21-day washout period, the alternative formulations were received. The blood samples were collected at 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14, 24, 36, 48, 72, 96, 120, 144, 168 h later. Liquid chromatography-tandem mass spectrometry (LC-MS/MS) was applied to determine the plasma concentrations of levamlodipine. Adverse events were recorded. Results: The 90% confidence intervals (CIs) of the ratio of geometric means (GMRs) of Cmax, AUC0-t, and AUC0-∞ under both fasted and fed conditions were within the prespecified bioequivalence limits between 80 ~ 125%. Under fasted conditions, 24 subjects were enrolled and completed the study. The mean Cmax was (2.70 ± 0.49) ng/mL, AUC0-t was (141.32 ± 36.24) ng × h/mL and AUC0-∞ was (157.14 ± 45.65) ng × h/mL after a single dose of 5 mg levamlodipine. The mean Cmax was (2.83 ± 0.52) ng/mL, AUC0-t was (153.62 ± 33.96) ng × h/mL and AUC0-∞ was (173.05 ± 41.78) ng × h/mL after a single dose of 10 mg amlodipine. Under fed conditions, 24 subjects were enrolled and completed the study. The mean Cmax was (2.73 ± 0.55) ng/mL, AUC0-t was (166.93 ± 49.96) ng × h/mL and AUC0-∞ was (190.99 ± 70.89) ng × h/mL after a single dose of 5 mg levamlodipine. The mean Cmax was (2.87 ± 0.81) ng/mL AUC0-t was (165.46 ± 43.58) ng × h/mL and AUC0-∞ was (189.51 ± 64.70) ng × h/mL after a single dose of 10 mg amlodipine. Serious adverse event was not observed. Conclusion: The trial confirmed that levamlodipine at a single dose of 5 mg and amlodipine at a single dose of 10 mg were bioequivalent under both fasted condition and fed condition. Trial registration: Cinicaltrials, NCT04411875 . Registered 3 June 2020 - Retrospectively registered.
Randomized, two-way crossover bioequivalence study of Levamlodipine besylate tablets in healthy Chinese subjects
Int J Clin Pharmacol Ther 2017 Oct;55(10):818-824.PMID:28619129DOI:10.5414/CP202998.
Objective: The present bioequivalence study was designed to compare the newly-developed Levamlodipine besylate 2.5-mg tablet (test) with that of its 2.5-mg marketed counterpart (reference) in healthy Chinese adult male volunteers. Methods: A single-dose, randomized, open-label, two-period, and two-treatment self-crossover study was conducted in healthy Chinese volunteers after informed consent was obtained. In each part of the study, the subjects were randomly assigned to receive the test or reference product (5 mg levamlodipine) in a 1 : 1 ratio, and then received the alternative product, following a 14-day washout period. Plasma levamlodipine concentrations were analyzed by liquid chromatography-tandem mass spectrometry. Pharmacokinetic parameters (noncompartmental model) were assessed with WinNonlin software. Analysis of variance (ANOVA) and FDA (USA) bioequivalence statistical criterion of 90% CI for 80 - 125% range (set at p ≤ 0.05) of geometric means ratios of test : reference product for Cmax, AUC0-t, and AUC0-∞ were determined. Tolerability was assessed during the entire study period. Results: ANOVA indicated that the period, sequence, and formulation had no significant effect on the PK parameters (p ≥ 0.05), although there was a statistically-significant difference between formulations in AUC0-t (p ≤ 0.05). The test formulation was bioequivalent to the marketed formulation as the 90% CI for the ratio of geometric means of Cmax (84.52 - 103.00%), AUC0-t (87.49 - 98.23%), and AUC0-∞ (84.30 - 103.25%) were within equivalence limits (80 - 125%) under fasting condition. No serious adverse events were found among the subjects. Conclusion: This study confirmed that test and reference Levamlodipine besylate tablets were bioequivalent under fasting condition. .
Effects of antihypertensive drugs losartan and Levamlodipine besylate on insulin resistance in patients with essential hypertension combined with isolated impaired fasting glucose
Hypertens Res 2016 May;39(5):321-6.PMID:26763851DOI:10.1038/hr.2015.155.
The objective of this study was to observe the antihypertensive effect of losartan and Levamlodipine besylate on insulin resistance in patients with essential hypertension (EH) combined with isolated impaired fasting glucose (i-IFG). Patients (n=244) were randomly assigned to losartan potassium tablets (50-100 mg per day) or Levamlodipine besylate tablets (2.5-5.0 mg per day) for intensive antihypertensive treatment with no lifestyle interventions for 3 years. The changes in fasting plasma glucose, fasting insulin (FINS) and insulin sensitivity index (ISI) from before to after treatment were observed. Blood pressure (BP) in each group was significantly reduced by treatment (P<0.05). After 12 months of treatment, the FINS level in the losartan potassium group was significantly decreased and ISI was significantly increased compared with before treatment (P<0.05) and compared with the Levamlodipine besylate group (P<0.05). After 24 and 36 months of treatment, FINS was significantly decreased and ISI was significantly improved in both groups compared with baseline (P<0.05), and there was no difference between the groups (P>0.05). The incidence of new-onset diabetes mellitus was not significantly different between two groups. The antihypertensive effect of losartan and Levamlodipine besylate could amoliorate insulin resistance in patients with EH combined with i-IFG. The improvement of insulin resistance by losartan potassium at 12 months might be better than that by Levamlodipine besylate; however, after 24 and 36 months of follow-up, both agents significantly alleviated insulin resistance. These results suggest that the effects of these two drugs on insulin resistance are not significantly different.