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| 250mg |
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| 500mg |
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Levamlodipine besylate, the besylate salt of Levamlodipine which is the S-isomer and impurity of Amlodipine (Amlodis; Amlor, Coroval; Lipinox; Norvasc; Amvaz), is an anti-hypertensive agent of the dihydropyridine (DHP) class and can be used for lowering blood pressure. It acts as a long-acting L-type calcium channel blocker (CCB).
| ln Vivo |
In a murine model of vascular dementia (VaD) induced by right unilateral common carotid arteries occlusion (rUCCAO), oral administration of Levamlodipine besylate at a dose of 0.1 mg/kg for eight weeks significantly reduced the escape latency to find the hidden platform during training trials in the Morris Water Maze test compared to the vehicle-treated group, indicating improved spatial learning. [1]
In the probe trial of the Morris Water Maze, no significant improvement in platform crossing times was observed in the Levamlodipine besylate-treated groups compared to the vehicle group. [1] In the Novel Object Recognition test, treatment with Levamlodipine besylate (0.1 or 0.5 mg/kg) significantly improved recognition memory in rUCCAO mice, as evidenced by increased exploring time and exploring frequency on the novel object compared to the vehicle-treated group. [1] Immunofluorescence staining revealed a significant decrease in phospho-CaMKII (Thr286) levels in the hippocampal CA1 region of vehicle-treated rUCCAO mice. Treatment with Levamlodipine besylate (0.1 mg/kg and 0.5 mg/kg) partially restored these decreased phospho-CaMKII levels. [1] Treatment with Levamlodipine besylate (0.1 mg/kg and 0.5 mg/kg) did not show significant effects on brain vascular structure, blood pressure, or the activation of astrocytes (GFAP, S100β expression) and microglia (Iba-1 expression) in the hippocampus of rUCCAO mice. [1] |
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| Animal Protocol |
Vascular dementia was induced in mice using the right unilateral common carotid arteries occlusion (rUCCAO) model. Mice were anesthetized, the right common carotid artery was isolated and double-ligated. Sham-operated mice underwent the same surgery without ligation. [1]
Eight weeks after the rUCCAO surgery, drug treatment began. Levamlodipine besylate was administered orally (p.o.) once daily at doses of 0.1 mg/kg or 0.5 mg/kg for a duration of eight weeks. The drug was dissolved in saline. The vehicle control group received oral saline. [1] Behavioral tests (Morris Water Maze and Novel Object Recognition Test) were conducted after the eight-week treatment period. [1] Following behavioral tests, mice were perfused, and brain tissues were collected for immunohistochemical analysis. [1] |
| References |
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| Additional Infomation |
Because levamlodipine besylate has L-type calcium channel blocking activity, which may lead to cerebral vasodilation and improved perfusion, it is considered a potential drug for the treatment of vascular dementia (VaD). [1] Studies have shown that the cognitive enhancement effect of low-dose levamlodipine besylate in VaD mouse models is not achieved by affecting blood pressure or neuroinflammation (astrocytocyte/microglia activation), but by restoring phosphorylation of CaMKII at Thr286 in the hippocampus, which is a key mediator of synaptic plasticity and memory. [1] This study used memantine (20 mg/kg, orally) as a positive control, and the results showed that memantine also had a restorative effect on phosphorylated CaMKII levels and cognitive function in VaD models. [1]
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| Molecular Formula |
C₂₆H₃₁CLN₂O₈S
|
|---|---|
| Molecular Weight |
567.05
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| Exact Mass |
566.149
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| CAS # |
150566-71-5
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| Related CAS # |
Levamlodipine;103129-82-4
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| PubChem CID |
11365087
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| Appearance |
White to light yellow solid powder
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| Density |
1.228 g/cm3
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| Boiling Point |
527.161ºC at 760 mmHg
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| Flash Point |
272.617ºC
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| LogP |
5.309
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
38
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| Complexity |
830
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CCOC(=O)C1=C(NC(=C([C@@H]1C2=CC=CC=C2Cl)C(=O)OC)C)COCCN.C1=CC=C(C=C1)S(=O)(=O)O
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| InChi Key |
ZPBWCRDSRKPIDG-LMOVPXPDSA-N
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| InChi Code |
InChI=1S/C20H25ClN2O5.C6H6O3S/c1-4-28-20(25)18-15(11-27-10-9-22)23-12(2)16(19(24)26-3)17(18)13-7-5-6-8-14(13)21;7-10(8,9)6-4-2-1-3-5-6/h5-8,17,23H,4,9-11,22H2,1-3H3;1-5H,(H,7,8,9)/t17-;/m0./s1
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| Chemical Name |
benzenesulfonic acid;3-O-ethyl 5-O-methyl (4S)-2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate
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| Synonyms |
Amlodis Amlor, Coroval Lipinox NorvascAmvaz (S)-Amlodipine besylate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 150 mg/mL (~264.53 mM)
H2O : ≥ 3.33 mg/mL (~5.87 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.41 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.41 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.41 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 | 3.5270 mL | |
| 10 mM | 0.1764 mL | 0.8818 mL | 1.7635 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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