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

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.

For research use only. We do not sell to patients.

Lercanidipine Chemical Structure

Lercanidipine Chemical Structure

CAS No. : 100427-26-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 129 In-stock
Solution
10 mM * 1 mL in DMSO USD 129 In-stock
Solid
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10 mg USD 155 In-stock
25 mg USD 295 In-stock
50 mg USD 450 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Lercanidipine:

Lercanidipine Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Lercanidipine

View All Calcium Channel Isoform Specific Products:

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

View All p38 MAPK Isoform Specific Products:

View All Isoforms
p38 MAPK p38α p38β MAPK13 p38δ p38γ

View All NF-κB Isoform Specific Products:

View All Isoforms
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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]
Cellular Effect
Cell Line Type Value Description References
LLC-MK2 IC50
434.99 μM
Compound: Lercanidipine
Cytotoxicity against rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay
Cytotoxicity against rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay
[PMID: 20934347]
LLC-MK2 IC50
8.43 μM
Compound: Lercanidipine
Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi infected in rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay
Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi infected in rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay
[PMID: 20934347]
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 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.), acute administration
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.
Clinical Trial
Molecular Weight

611.73

Formula

C36H41N3O6
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (163.47 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 1.6347 mL 8.1735 mL 16.3471 mL
5 mM 0.3269 mL 1.6347 mL 3.2694 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

  • Protocol 1

    dissolve in 20% ethanol, 20% DMSO and 60% normal saline

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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.65%

SDS (251 KB)

COA (252 KB) HNMR (291 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
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 (protect from 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
DMSO 1 mM 1.6347 mL 8.1735 mL 16.3471 mL 40.8677 mL
5 mM 0.3269 mL 1.6347 mL 3.2694 mL 8.1735 mL
10 mM 0.1635 mL 0.8174 mL 1.6347 mL 4.0868 mL
15 mM 0.1090 mL 0.5449 mL 1.0898 mL 2.7245 mL
20 mM 0.0817 mL 0.4087 mL 0.8174 mL 2.0434 mL
25 mM 0.0654 mL 0.3269 mL 0.6539 mL 1.6347 mL
30 mM 0.0545 mL 0.2725 mL 0.5449 mL 1.3623 mL
40 mM 0.0409 mL 0.2043 mL 0.4087 mL 1.0217 mL
50 mM 0.0327 mL 0.1635 mL 0.3269 mL 0.8174 mL
60 mM 0.0272 mL 0.1362 mL 0.2725 mL 0.6811 mL
80 mM 0.0204 mL 0.1022 mL 0.2043 mL 0.5108 mL
100 mM 0.0163 mL 0.0817 mL 0.1635 mL 0.4087 mL
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Lercanidipine 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:

Lercanidipine100427-26-7Calcium ChannelApoptosisReactive Oxygen Speciesp38 MAPKNF-κBCa2+ channelsCa channelsNuclear factor-κBNuclear factor-kappaBanti-oxidantanti-inflammatoryanti-apoptoticanti-hypertensiveCalcium channel blockerrenoprotectiveneuroprotectivestrokeMCAo modelVSMCSHRInhibitorinhibitorinhibit

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