2. Membrane Transporter/Ion Channel Neuronal Signaling Apoptosis Immunology/Inflammation NF-κB Metabolic Enzyme/Protease MAPK/ERK Pathway
  3. Calcium Channel Apoptosis Reactive Oxygen Species p38 MAPK NF-κB
  4. Lercanidipine hydrochloride

Lercanidipine hydrochloride 

Art. -Nr.: HY-B0612A Reinheit: 99.80%
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Lercanidipine is a third-generation, lipophilic, brain-penetrant, vascular-selective and orally active dihydropyridine-calcium channel blocker with a pIC50 of 7.74 (converts from μM). Lercanidipine has long lasting antihypertensive action as well as reno- and neuro-protective effect. Lercanidipine also shows anti-oxidant, anti-inflammatory and anti-apoptotic properties. Lercanidipine can be used in cardiovascular and neurological research.

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Lercanidipine hydrochloride Chemische Struktur

Lercanidipine hydrochloride Chemische Struktur

CAS. Nr. : 132866-11-6

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10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 61 Auf Lager
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Based on 1 publication(s) in Google Scholar

Other Forms of Lercanidipine hydrochloride:

Lercanidipine hydrochloride Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Lercanidipine hydrochloride

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Beschreibung

Lercanidipine is a third-generation, lipophilic, brain-penetrant, vascular-selective and orally active dihydropyridine-calcium channel blocker with a pIC50 of 7.74 (converts from μM). Lercanidipine has long lasting antihypertensive action as well as reno- and neuro-protective effect. Lercanidipine also shows anti-oxidant, anti-inflammatory and anti-apoptotic properties. Lercanidipine can be used in cardiovascular and neurological research[1][2][3][4][5].

IC50 & Target

calcium channel[1]
In Vitro

Lercanidipine (1, 10 μM, 24 h) exerts suppression of NO, ROS and TNF-a through down-regulation of iNOS, MMP-2/MMP-9, and HMGB1, as well as inhibition of MAPKs, Akt/IkB-a and NF-kB pathways in LPS/IFN-γ-induced VSMCs[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Lercanidipine hydrochloride Related Antibodies

Western Blot Analysis[3]

Cell Line: LPS/IFN-γ-induced VSMC
Concentration: 1 and 10 μM
Incubation Time: 24 h
Result: Down-regulated LPS/IFN-γ-induced iNOS, MMP-2/-9, NF-kB expression and IkB-a phosphorylation. Decreased cytosolic HMGB1 fraction and extracellular HMGB1 release while increasing nuclear HMGB1 fraction.
In Vivo

Lercanidipine (1, 0.5 and 0.25 mg/kg, i.p., acute administration) significantly reduces neurological deficit score, motor deficits and cerebral infarction volume in the MCAo model rats[3].
Lercanidipine (1.92-0.12 mg/kg, p.o., acute administration) lowers blood pressure effectively and dose-dependently in spontaneous hypertensive rats[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Albino male Wistar rats, middle cerebral artery occlusion (MCAo) model[3]
Dosage: 1, 0.5 and 0.25 mg/kg
Administration: Intraperitoneal injection (i.p.), acute administration
Result: Showed neuroprotective effect in focal cerebral ischemic-reperfusion injury model, most effective dose was found to be at 0.5 mg/kg.
Significantly attenuated percentage infarct volume, significantly improved the apparent diffusion coefficient.
Declined MMP-9 activity significantly in all Lercanidipine treated groups till 240 min post-reperfusion, while MMP-2 activity was inhibited only till 120 min post-reperfusion.
Decreased caspase-3 activity significantly in Lercanidipine 15 and 120 min post-reperfusion groups only. Exhibited significant reduction in caspase-9 activity in all groups except at 240 min post-reperfusion group.
Animal Model: Male SHRs [4]
Dosage: 1.92, 0.96, 0.48, 0.24 and 0.12 mg/kg
Administration: Oral gavage (p.o.) for once
Result: Increased the AOC values of mean arterial pressure in a dose-dependent manner (285.4 mmHg×hour for 1.92 mg) as well as decreased BP.
Klinische Studie
Molekulargewicht

648.19

Formel

C36H42ClN3O6
CAS. Nr.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=C(C)NC(C)=C(C(OC)=O)C1C2=CC=CC([N+]([O-])=O)=C2)OC(C)(C)CN(CCC(C3=CC=CC=C3)C4=CC=CC=C4)C.[H]Cl
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

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

Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 50 mg/mL (77.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5428 mL 7.7138 mL 15.4276 mL
5 mM 0.3086 mL 1.5428 mL 3.0855 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molaritätsrechner

  • Verdünnungsrechner

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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 (3.86 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.
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)

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.
Reinheit & Dokumentation
Verweise

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). 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 1.5428 mL 7.7138 mL 15.4276 mL 38.5689 mL
5 mM 0.3086 mL 1.5428 mL 3.0855 mL 7.7138 mL
10 mM 0.1543 mL 0.7714 mL 1.5428 mL 3.8569 mL
15 mM 0.1029 mL 0.5143 mL 1.0285 mL 2.5713 mL
20 mM 0.0771 mL 0.3857 mL 0.7714 mL 1.9284 mL
25 mM 0.0617 mL 0.3086 mL 0.6171 mL 1.5428 mL
30 mM 0.0514 mL 0.2571 mL 0.5143 mL 1.2856 mL
40 mM 0.0386 mL 0.1928 mL 0.3857 mL 0.9642 mL
50 mM 0.0309 mL 0.1543 mL 0.3086 mL 0.7714 mL
60 mM 0.0257 mL 0.1286 mL 0.2571 mL 0.6428 mL
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Lercanidipine hydrochloride Related Classifications

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:

Lercanidipine132866-11-6Calcium ChannelApoptosisReactive Oxygen Speciesp38 MAPKNF-κBCa2+ channelsCa channelsNuclear factor-κBNuclear factor-kappaBanti-oxidantanti-inflammatoryanti-apoptoticanti-hypertensiveCalcium channel blockerrenoprotectiveneuroprotectivestrokeMCAo modelVSMCSHRInhibitorinhibitorinhibit

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