Art. -Nr.: HY-14744

Levamlodipine

(Synonyms: (S)-Amlodipine; Levoamlodipine)

2 Cited Publications

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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.

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Reinheit: 98.06%
CAS. Nr.: 103129-82-4
Formel: C₂₀H₂₅ClN₂O₅
Molecular Weight:408.88

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Levamlodipine Chemical Structure

CAS. Nr.: 103129-82-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
- Clinical Trial
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

L-type calcium channel

MMP-9

Alle Calcium Channel Isoform-spezifische Produkte anzeigen :

Alle MMP Isoform-spezifische Produkte anzeigen :

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.

Parmacokinetics

Species	Dose	Route	C_max	T_max	T_1/2	AUC_0-t	MRT_0-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 C_maxof 182.27 ng/mL at t_max of 36 hours, t_1/2 of 23.55 hours, and AUC_0-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 A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 103129-82-4
Appearance Solid
Molecular Weight 408.88
Formel 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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (2)

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Journal Impact Factor

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

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4457 mL

12.2285 mL

24.4571 mL

5 mM

0.4891 mL

2.4457 mL

4.8914 mL

10 mM

0.2446 mL

1.2229 mL

2.4457 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Aidong Z, et al. Levamlodipine besylate influence on intimal hyperplasia and plaque stability after balloon injury in rabbits[J]. J Clin Cardiol, 2015, 31(1): 101-105.

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Levamlodipine

2 Cited Publications

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Levamlodipine

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Publications Citing Use of MedChemExpress (MCE) Levamlodipine

Alle Calcium Channel Isoform-spezifische Produkte anzeigen

Alle MMP Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Levamlodipine Related Classifications

HY-14744 Related Classifications