2. Membrane Transporter/Ion Channel Neuronal Signaling Metabolic Enzyme/Protease
  3. Calcium Channel MMP
  4. Levamlodipine

Levamlodipine  (Synonyms: (S)-Amlodipine; Levoamlodipine)

Cat. No.: HY-14744 Purity: 98.06%
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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.

Levamlodipine

Levamlodipine Chemical Structure

CAS No. : 103129-82-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 2 publication(s) in Google Scholar

Other Forms of Levamlodipine:

Levamlodipine Related Antibodies

Top Publications Citing Use of Products

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

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MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8 MMP-19

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2][3].
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.

Levamlodipine Related Antibodies
Parmacokinetics
Species Dose Route Cmax Tmax T1/2 AUC0-t MRT0-t Bioavailability
Rat[3] 2 mg/kg i.v. 156.90 ± 17.75 ng/mL 0.083 ± 0.00 h 5.12 ± 0.62 h 516.45 ± 80.15 ng·h/mL 7.98 ± 0.32 h /
Rat[3] 4 mg/kg p.o. 40.50 ± 6.50 ng/mL 4 ± 1.15 h 8.80 ± 1.87 h 1324.75 ± 139.21 ng·h/mL 36.78 ± 0.96 h 42.78 %
In Vivo

Levamlodipine (2.5 mg/d; intragastric administration; once daily; for 8 consecutive weeks) exerts no significant inhibitory effect on intimal hyperplasia after balloon-induced endothelial injury of the abdominal aorta in rabbits, but it can improve plaque stability by reducing the expression of MMP-9 in plaques. Meanwhile, the serum LDL-C level shows a decreasing trend, while the serum TNF-α level increases significantly[1].
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
Molecular Weight

408.88

Formula

C20H25ClN2O5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=C(COCCN)NC(C)=C(C(OC)=O)[C@@H]1C2=CC=CC=C2Cl)OCC
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
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4457 mL 12.2285 mL 24.4571 mL
5 mM 0.4891 mL 2.4457 mL 4.8914 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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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.

  • Protocol 1

    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.
  • Protocol 2

    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:

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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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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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
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Levamlodipine Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Levamlodipine103129-82-4(S)-Amlodipine LevoamlodipineCalcium ChannelMMPCa2+ channelsCa channelsMatrix metalloproteinasesL-type calcium channelatherosclerotic plaquesMMP-9porcine skinrabbitmale SHRatherosclerosislow-density lipoprotein cholesterolhypertensionbisoprololInhibitorinhibitorinhibit

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