Cat. No.: HY-B0612

Lercanidipine

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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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Pureté: 99.93%
CAS No.: 100427-26-7
Formule: C₃₆H₄₁N₃O₆
Masse moléculaire:611.73

Stockage:

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

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

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

calcium channel^[1]

Voir tous les produits spécifiques à Isoform Calcium Channel :

Voir tous les produits spécifiques à Isoform p38 MAPK :

Voir tous les produits spécifiques à Isoform NF-κB :

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
Masse moléculaire 611.73
Formule 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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, protect from light

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

Publications (1)

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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

Solvant et solubilité

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (282 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
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Instruction de manipulation (2659 KB)

Références

[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

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Lercanidipine

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Publications Citing Use of MedChemExpress (MCE) Lercanidipine

Voir tous les produits spécifiques à Isoform Calcium Channel

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Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

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