Cat. No.: HY-B0612

Lercanidipine

1 Cited Publications

Customer Review

Based on 1 publication(s) in Google Scholar

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.

Purity: 99.93%
CAS No.: 100427-26-7
Formula: C₃₆H₄₁N₃O₆
Molecular Weight:611.73

Storage:

4°C, protect from light

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

Lercanidipine Chemical Structure

CAS No.: 100427-26-7

Size

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

calcium channel^[1]

All Calcium Channel Isoforms :

All p38 MAPK Isoforms :

All NF-κB Isoforms :

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.

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.

Chemical Information

CAS No. 100427-26-7
Appearance Solid
Molecular Weight 611.73
Formula C₃₆H₄₁N₃O₆
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)

Publications (1)

All

Sort by:

Journal Impact Factor

Cell Calcium

Mutations and clinical significance of calcium voltage-gated channel subunit alpha 1E (CACNA1E) in non-small cell lung cancer. [Abstract]

2022 Mar:102:102527. PMID: 35026540

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)

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

1.6347 mL

8.1735 mL

16.3471 mL

5 mM

0.3269 mL

1.6347 mL

3.2694 mL

10 mM

0.1635 mL

0.8174 mL

1.6347 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 (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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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 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.

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (557 KB)
- English - EN (557 KB)
- Français - FR (557 KB)
- Deutsch - DE (557 KB)
- Norwegian - NO (557 KB)
- Español - ES (557 KB)
- Swedish - SV (557 KB)
- Italian - IT (557 KB)
- Korean - KR (557 KB)
- Portuguese - PT (557 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)

References

[1]. Barrios, V., et al., Lercanidipine is an effective and well tolerated antihypertensive drug regardless the cardiovascular risk profile: The LAURA study. Int J Clin Pract, 2006. 60(11): p. 1364-70. [Content Brief]

[2]. Duda-Seiman D, et al. Calcium Channel Blockers--Benefits Upon Vascular Biology in Hypertensive Patients. Cardiovasc Hematol Agents Med Chem. 2015;13(1):54-62. [Content Brief]

[3]. Gupta S, et al. Neuroprotective effect of lercanidipine in middle cerebral artery occlusion model of stroke in rats. Exp Neurol. 2017 Feb;288:25-37. [Content Brief]

[4]. Yeh JL, et al. Lercanidipine and labedipinedilol--A attenuate lipopolysaccharide/interferon-γ-induced inflammation in rat vascular smooth muscle cells through inhibition of HMGB1 release and MMP-2, 9 activities. Atherosclerosis. 2013 Feb;226(2):364-72. [Content Brief]

[5]. Lee JJ, et al. Drug synergism of antihypertensive action in combination of telmisartan with lercanidipine in spontaneous hypertensive rats. Arch Pharm Res. 2010 Sep;33(9):1411-8. [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

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

Lercanidipine

1 Cited Publications

100 mg Get Quote

Subscribe to the

MedChemExpress

Newsletter

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

Lercanidipine

Antioxidant Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Anti-Cardiovascular Disease Compound Library

NMPA-Approved Drug Library

Pyroptosis Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Neuroprotective Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Transcription Factor-Targeted Library

Anti-Liver Cancer Compound Library

Antidepressant Compound Library

Calcium Channel Blocker Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Off-patent Drug Library

Antihypertensive Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Ion Channel Compound Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

FDA Kinase Inhibitor Library

RNA Binding Bioactive Compound Library

Lactylation Compound Library

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Membrane Transporter/Ion Channel Compound Library

Metabolism/Protease Compound Library

Neuronal Signaling Compound Library

NF-κB Signaling Compound Library

Stem Cell Signaling Compound Library

FDA-Approved Drug Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Publications Citing Use of MedChemExpress (MCE) Lercanidipine

All Calcium Channel Isoforms

All p38 MAPK Isoforms

All NF-κB Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References