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

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

製品番号: HY-14744A 純度: 99.84%
COA 取扱説明書 Technical Support

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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Levamlodipine besylate

Levamlodipine besylate 構造式

CAS 番号 : 150566-71-5

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 40 在庫あり
Solution
10 mM * 1 mL in DMSO USD 40 在庫あり
Solid
5 mg $32 在庫あり
10 mg $45 在庫あり
25 mg $80 在庫あり
50 mg $112 在庫あり
100 mg $155 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 2 publication(s) in Google Scholar

Other Forms of Levamlodipine besylate:

Levamlodipine besylate 関連抗体

Top Publications Citing Use of Products

Calcium Channel アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

MMP アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
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

  • 生物活性

  • 純度とドキュメンテーション

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製品説明

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[1][2][3].
IC50 & Target

Calcium channel[1].
体外実験

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.

Levamlodipine besylate 関連抗体

Cell Viability Assay[4].

Cell Line: Neuronal cell
Concentration: 0-50 μM
Incubation Time: 2 h
Result: Inhibited cell viability at concentrations greater than 5 μM.
体内実験

Levamlodipine (2.5 mg/d; intragastric administration; once daily; for 8 consecutive weeks) besylate 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) 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.

Animal Model: Spontaneously hypertensive rats (SHR)[3].
Dosage: 1 mg/kg
Administration: Oral gavage (p.o.); once daily; 16 weeks
Result: Reduced systolic blood pressure (SBP) and diastolic blood pressure (DBP), reduced heart and aortic hypertrophy, increased kidney weight to prevent kidney atrophy.
Animal Model: VaD mice model of right unilateral common carotid arteries occlusion (rUCCAO)[1].
Dosage: 0.1, 0.5 mg/kg
Administration: Oral gavage (p.o.); once daily; 8 weeks
Result: Recovered phosphorylated CaMKII (Thr286) levels in the hippocampus and improved cognitive impairment in mice.
分子量

567.05

分子式

C26H31ClN2O8S
CAS 番号
Appearance

Solid

Color

White to light yellow

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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

-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)
溶剤 & 溶解度
体外: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 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
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 (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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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 (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.
  • Protocol 2

    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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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.
純度とドキュメンテーション

純度: 99.84%

COA (258 KB) RP-HPLC (258 KB) MS (177 KB)

取扱説明書 (2659 KB)
参考文献

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.

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Levamlodipine besylate Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • 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:

Levamlodipine besylate150566-71-5(S)-Amlodipine besylate Levoamlodipine besylateCalcium ChannelMMPCa2+ channelsCa channelsMatrix metalloproteinasescalcium channelvasodilationhypertensioncerebrovascularInhibitorinhibitorinhibit

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