Cat. No.: HY-B0612A

Lercanidipine hydrochloride

1 Cited Publications

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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.: 132866-11-6
Formula: C₃₆H₄₂ClN₃O₆
Molecular Weight:648.19

Storage:

4°C, sealed storage, away from moisture

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

Lercanidipine hydrochloride Chemical Structure

CAS No.: 132866-11-6

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
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 :

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.) 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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 132866-11-6
Appearance Solid
Molecular Weight 648.19
Formula C₃₆H₄₂ClN₃O₆
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Publications (1)

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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 : 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)

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

1.5428 mL

7.7138 mL

15.4276 mL

5 mM

0.3086 mL

1.5428 mL

3.0855 mL

10 mM

0.1543 mL

0.7714 mL

1.5428 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 (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.

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:

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 (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.

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

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	1.5428 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

Lercanidipine hydrochloride

1 Cited Publications

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Lercanidipine hydrochloride

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Publications Citing Use of MedChemExpress (MCE) Lercanidipine hydrochloride

All Calcium Channel Isoforms

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Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation