Levamlodipine besylate
Based on 2 publication(s) in Google Scholar
Levamlodipine ((S)-Amlodipine; Levoamlodipin) besylate is an orally active L-type calcium channel blocker and MMP-9 modulator with high permeability and retention properties. Levamlodipine besylate significantly enhances plaque stability and improves lipid profiles by reducing blood pressure, decreasing systolic blood pressure variability, and inhibiting MMP-9 expression in atherosclerotic plaques. Levamlodipine besylate not only alleviates cardiac and aortic hypertrophy and prevents renal atrophy, but also produces synergistic effects in blood pressure reduction and organ protection when combined with bisoprolol (HY-129029). Levamlodipine besylate exerts no significant inhibitory effect on abdominal aortic intimal hyperplasia. When excessively accumulated in the epidermis, Levamlodipine besylate may induce changes in keratin structure, impair the skin barrier and trigger inflammation; long-term use further exacerbates skin irritation caused by local administration. Levamlodipine besylate can be used in research related to hypertension and atherosclerosis.
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- Pureté : 99.84%
- CAS No.: 150566-71-5
- Formule: C26H31ClN2O8S
- Masse moléculaire:567.05
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Stockage:
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Levamlodipine besylate
MoreVoir tous les produits spécifiques à Isoform Calcium Channel
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Activité biologique
Description
IC50 & Target
Calcium channel[1].
In Vitro
Levamlodipine besylate-Sorbic acid (HY-N0626) ion pair patches (13-15% (w/w) LAM-SA, 10% (w/w) IPM; 72 h) maintain equivalent porcine skin permeability to free levamlodipine patches, and addition of 10% IPM significantly enhances permeability; the optimized 13% LAM-SA, 10% IPM, 70 μm patch achieves high, predictable transdermal delivery over 72 h[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Neuronal cell
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Concentration:0-50 μM
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Incubation Time:2 h
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Result:Inhibited cell viability at concentrations greater than 5 μM.
In Vivo
Levamlodipine (1-4 mg/kg; intragastric administration; single dose; 1 mg/kg/day; p.o.; daily; 16 weeks) besylate reduces blood pressure in male SHR in a dose-dependent manner[2].
The ion-pair transdermal patch of Levamlodipine besylate and sorbic acid (HY-N0626) (12-15% w/w; transdermal administration; single dose; 72 h) significantly reduces skin irritation in rabbits. Compared with non-ion-pair levamlodipine patches, it shows a lower erythema index, milder epidermal thickening, and faster skin recovery[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Spontaneously hypertensive rats (SHR)[3].
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Dosage:1 mg/kg
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Administration:Oral gavage (p.o.); once daily; 16 weeks
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Result:Reduced systolic blood pressure (SBP) and diastolic blood pressure (DBP), reduced heart and aortic hypertrophy, increased kidney weight to prevent kidney atrophy.
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Animal Model:VaD mice model of right unilateral common carotid arteries occlusion (rUCCAO)[1].
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Dosage:0.1, 0.5 mg/kg
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Administration:Oral gavage (p.o.); once daily; 8 weeks
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Result:Recovered phosphorylated CaMKII (Thr286) levels in the hippocampus and improved cognitive impairment in mice.
- RNA extraction experimental
- Mitochondrial membrane-potential fluorescent assay
- Mitochondrial membrane-potential and mitochondrial mass staining
- Transepithelial/transendothelial electrical resistance assay
- Research Protocol for Cardiovascular Diseases
- Research Protocol for Inflammation-related Diseases
- Dermal Irritation/Dermal Toxicity Study
Chemical Information
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CAS No. 150566-71-5
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Appearance Solid
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Masse moléculaire 567.05
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Formule C26H31ClN2O8S
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Color White to light yellow
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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
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Synonyms
(S)-Amlodipine besylate; Levoamlodipine besylate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (2)
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Journal Impact Factor
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Most Recent
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Cell
Structural basis for human Cav1.2 inhibition by multiple drugs and the neurotoxin calciseptine. [Abstract]2023 Nov 22;186(24):5363-5374.e16. PMID: 37972591 -
Proc Natl Acad Sci U S A
Design and structural basis of selective 1,4-dihydropyridine inhibitors of the calcium-activated potassium channel KCa3.1. [Abstract]2025 May 6;122(18):e2425494122. PMID: 40294255
Solvant et solubilité
In Vitro:
DMSO : ≥ 150 mg/mL (264.53 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 3.33 mg/mL (5.87 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.41 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.41 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (285 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Instruction de manipulation (2659 KB)
Références
[2]. Yang YL, et al. Synergic effects of levamlodipine and bisoprolol on blood pressure reduction and organ protection in spontaneously hypertensive rats. CNS Neurosci Ther. 2012;18(6):471-474. [Content Brief]
[3]. Wu J, et al. Development of levamlodipine long-acting patches based on an ion-pair strategy: Investigation of the mechanism for reducing skin irritation. Int J Pharm. 2024;665:124703. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.7635 mL | 8.8176 mL | 17.6351 mL | 44.0878 mL |
| 5 mM | 0.3527 mL | 1.7635 mL | 3.5270 mL | 8.8176 mL | |
| DMSO | 10 mM | 0.1764 mL | 0.8818 mL | 1.7635 mL | 4.4088 mL |
| 15 mM | 0.1176 mL | 0.5878 mL | 1.1757 mL | 2.9392 mL | |
| 20 mM | 0.0882 mL | 0.4409 mL | 0.8818 mL | 2.2044 mL | |
| 25 mM | 0.0705 mL | 0.3527 mL | 0.7054 mL | 1.7635 mL | |
| 30 mM | 0.0588 mL | 0.2939 mL | 0.5878 mL | 1.4696 mL | |
| 40 mM | 0.0441 mL | 0.2204 mL | 0.4409 mL | 1.1022 mL | |
| 50 mM | 0.0353 mL | 0.1764 mL | 0.3527 mL | 0.8818 mL | |
| 60 mM | 0.0294 mL | 0.1470 mL | 0.2939 mL | 0.7348 mL | |
| 80 mM | 0.0220 mL | 0.1102 mL | 0.2204 mL | 0.5511 mL | |
| 100 mM | 0.0176 mL | 0.0882 mL | 0.1764 mL | 0.4409 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Levamlodipine besylate Related Classifications
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