Levamlodipine
Based on 2 publication(s) in Google Scholar
Levamlodipine ((S)-Amlodipine; Levoamlodipin) is an orally active L-type calcium channel blocker and MMP-9 modulator with high permeability and retention properties. Levamlodipine 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 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 exerts no significant inhibitory effect on abdominal aortic intimal hyperplasia. When excessively accumulated in the epidermis, Levamlodipine 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 can be used in research related to hypertension and atherosclerosis.
For research use only. We do not sell to patients.
- Purity : 98.06%
- CAS No.: 103129-82-4
- Formula: C20H25ClN2O5
- Molecular Weight:408.88
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
-
HY-B0424
NitrendipineCalcium Channel Blocker -
HY-17404
CilnidipineCa Channel Blocker -
HY-17402
NisoldipineCalcium Channel Blocker -
HY-B0023
AzelnidipineCalcium Channel Blocker -
HY-B0317B
Amlodipine besylateCalcium Channel Blocker -
HY-B0317BR
Amlodipine (besylate) (Standard)Calcium Channel Blocker -
HY-B0284
NifedipineCalcium Channel Antagonist -
HY-B0265
NimodipineDihydropyridine Calcium Antagonist -
HY-N0504
LovastatinHMG-CoA Inhibitor -
HY-B0309
FelodipineCalcium Channel Antagonist -
HY-B0216
EthinylestradiolEndogenous Metabolite -
HY-B0214
PrednisoneGlucocorticoid Receptor Agonist
Publications Citing Use of MedChemExpress (MCE) Levamlodipine
MoreAll Calcium Channel Isoforms
More
Biological Activity
Description
IC50 & Target
|
L-type calcium channel |
MMP-9 |
In Vitro
Levamlodipine-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. Further protocols information, click here.
Parmacokinetics
In Vivo
Levamlodipine (1-4 mg/kg; intragastric administration; single dose; 1 mg/kg/day; p.o.; daily; 16 weeks) reduces blood pressure in male SHR in a dose-dependent manner[2].
The ion-pair transdermal patch of Levamlodipine 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.
-
Animal Model:New Zealand rabbit (5~6 months old, male, 2.0~2.5 kg; induced by high-fat diet feeding + abdominal aortic balloon endothelial injury)[1]
-
Dosage:2.5 mg/d
-
Administration:p.o. (mixed with feed); once daily; 8 weeks
-
Result:Showed a decreasing trend in serum LDL-C level (16.24 mmol/L vs model group 19.41 mmol/L, P=0.08).
Resulted in abdominal aortic plaque thickness of 313.56 μm and intimal hyperplasia index (IHI) of 0.66, with no significant difference compared to model group (405.93 μm, 0.68, P>0.05).
Showed no significant difference in serum hs-CRP, LP-PLA2, PAI-1 levels compared to model group (P>0.05).
Increased serum TNF-α level to 113.11 μg/mL, which was significantly higher than model group's 81.13 μg/mL (P<0.05).
Reduced the positive expression area percentage of MMP-9 in plaques to 52.45%, which was significantly lower than model group's 70.84% (P<0.05).
-
Animal Model:Japanese white rabbits (male, 1.8-2.2 kg)[3]
-
Dosage:12% w/w LAM-SA (6 cm2 skin area); 13.00% w/w LAM-SA (1.13 cm2 skin area); 15% w/w LAM-SA
-
Administration:topical; single exposure; 72 hours
-
Result:Produced post-removal erythema index of 188 at 1 hour, 181 at 24 hours, and 166 at 72 hours for 13% w/w formulation; showed significantly lower ΔEI than non-ion-paired LAM patch at all time points (p < 0.05).
Exhibited only slight epidermal thickening with no inflammatory cell infiltration, and significantly lower epidermal thickness than non-ion-paired LAM patch for 13% w/w formulation.
Produced only mild erythema, with the lowest erythema index among all tested ion-paired formulations for 15% w/w formulation.
-
Animal Model:Wistar rats (male, 180-220 g)[3]
-
Dosage:12% w/w LAM-SA (6 cm2 skin area)
-
Administration:topical; single exposure
-
Result:Achieved Cmax of 182.27 ng/mL at tmax of 36 hours, t1/2 of 23.55 hours, and AUC0-t of 7863.22h·ng/mL.
Reached absolute bioavailability of 81.20%.
Maintained detectable plasma levamlodipine concentrations for at least 4 days, with complete elimination by the fifth day.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 103129-82-4
-
Appearance Solid
-
Molecular Weight 408.88
-
Formula C20H25ClN2O5
-
Color White to off-white
-
SMILES
O=C(C1=C(COCCN)NC(C)=C(C(OC)=O)[C@@H]1C2=CC=CC=C2Cl)OCC
-
Synonyms
(S)-Amlodipine; Levoamlodipine
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
-
Journal Impact Factor
-
Most Recent
-
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
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (244.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (6.11 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 (6.11 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:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
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.
Protocols
-
RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
-
Mitochondrial membrane-potential fluorescent assay
Mitochondrial membrane potential fluorescent assays estimate ΔΨm in living cells using lipophilic cationic dyes such as TMRM, TMRE, rhodamine 123, and JC-1, which accumulate in mitochondria according to membrane polarization; loss of signal after FCCP or CCCP treatment is interpreted as mitochondrial depolarization. TMRM/TMRE and rhodamine 123 are commonly used for semi-quantitative live-cell microscopy or flow cytometry, while JC-1 can report a shift from red aggregate fluorescence to green monomer fluorescence during depolarization; interpretation requires controls because dye concentration, quenching mode, cell type, dye efflux, and mitochondrial mass can affect fluorescence independently of ΔΨm.
-
Mitochondrial membrane-potential and mitochondrial mass staining
Mitochondrial membrane potential staining measures the electrochemical polarization across the mitochondrial inner membrane in live cells using lipophilic cationic fluorescent probes; early rhodamine-based work showed that selective mitochondrial dye accumulation is lost when the mitochondrial transmembrane potential is dissipated. JC-1 reports mitochondrial polarization by shifting from green monomer fluorescence to red J-aggregate fluorescence as dye concentration increases within energized mitochondria; therefore, the red/green fluorescence ratio is used as a relative readout of mitochondrial membrane potential. TMRE or TMRM staining provides a single-channel relative readout because these cationic rhodamine esters accumulate in polarized mitochondria, and lower fluorescence indicates reduced mitochondrial polarization when acquisition and dye-loading conditions are controlled. Mitochondrial mass staining is commonly performed with MitoTracker Green FM or related MitoTracker dyes as
-
Transepithelial/transendothelial electrical resistance assay
TEER measures electrical resistance across epithelial or endothelial monolayers cultured on permeable supports, and the readout reflects ionic conductance through the cell barrier, especially the paracellular pathway regulated by junctional integrity. TEER can be measured without destroying the monolayer and is commonly used before or during transport, permeability, barrier-disruption, and barrier-maturation experiments. TEER values are influenced by biological maturation and technical conditions; reported factors include temperature, medium formulation, passage number, electrode geometry, membrane properties, and junctional length during early monolayer maturation. Therefore, TEER should be interpreted with blank-insert subtraction, area normalization, repeated readings, and, when possible, orthogonal barrier readouts such as FITC-dextran flux or tight-junction staining.
-
Research Protocol for Cardiovascular Diseases
Cardiovascular disease can be modeled as maladaptive cardiac remodeling, where ischemic injury or pressure overload activates inflammatory signaling, fibroblast activation, extracellular-matrix deposition, cardiomyocyte hypertrophy, vascular remodeling, and progressive ventricular dysfunction. The TGF-β/SMAD axis is a central profibrotic pathway after myocardial injury and pressure overload, while innate immune and cytokine pathways regulate leukocyte recruitment, scar formation, and adverse remodeling. Key unresolved questions include which inflammatory signals are reparative versus harmful, when fibrosis is protective versus maladaptive, and whether pathway inhibition improves function without weakening necessary infarct healing or compensatory remodeling.
-
Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
-
Dermal Irritation/Dermal Toxicity Study
This protocol assesses dermal irritation using reconstructed human epidermis (RhE) models such as EpiDerm, EPISKIN, and SkinEthic RHE, in which a test substance is applied topically and tissue viability is measured after exposure; reduced viability reflects cytotoxic injury associated with skin irritation potential. The primary readout is MTT reduction, where viable cells convert tetrazolium salt into colored formazan measured by spectrophotometry; this signal is used as a quantitative viability endpoint for classifying irritant versus non-irritant responses. The historical in vivo comparator is the Draize rabbit skin irritation method, which scores erythema and edema after topical exposure, but validated RhE assays were developed to replace or reduce reliance on this animal-based endpoint.
Purity & Documentation
-
Data Sheet (283 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
References
[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. 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4457 mL | 12.2285 mL | 24.4571 mL | 61.1426 mL |
| 5 mM | 0.4891 mL | 2.4457 mL | 4.8914 mL | 12.2285 mL | |
| 10 mM | 0.2446 mL | 1.2229 mL | 2.4457 mL | 6.1143 mL | |
| 15 mM | 0.1630 mL | 0.8152 mL | 1.6305 mL | 4.0762 mL | |
| 20 mM | 0.1223 mL | 0.6114 mL | 1.2229 mL | 3.0571 mL | |
| 25 mM | 0.0978 mL | 0.4891 mL | 0.9783 mL | 2.4457 mL | |
| 30 mM | 0.0815 mL | 0.4076 mL | 0.8152 mL | 2.0381 mL | |
| 40 mM | 0.0611 mL | 0.3057 mL | 0.6114 mL | 1.5286 mL | |
| 50 mM | 0.0489 mL | 0.2446 mL | 0.4891 mL | 1.2229 mL | |
| 60 mM | 0.0408 mL | 0.2038 mL | 0.4076 mL | 1.0190 mL | |
| 80 mM | 0.0306 mL | 0.1529 mL | 0.3057 mL | 0.7643 mL | |
| 100 mM | 0.0245 mL | 0.1223 mL | 0.2446 mL | 0.6114 mL |
Levamlodipine Related Classifications
HY-14744 Related Classifications
Powered by Bioz