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

Lercanidipine hydrochloride 

Cat. No.: HY-B0612A Purity: 99.80%
COA Handling Instructions

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 hydrochloride Chemical Structure

Lercanidipine hydrochloride Chemical Structure

CAS No. : 132866-11-6

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Solid + Solvent
10 mM * 1 mL in DMSO
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Solid
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10 mg USD 55 In-stock
50 mg USD 209 In-stock
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200 mg USD 429 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Lercanidipine hydrochloride:

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  • 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]

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
Molecular Weight

648.19

Formula

C36H42ClN3O6

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.[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)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (77.14 mM; Need ultrasonic)

H2O : 1 mg/mL (1.54 mM; ultrasonic and warming and heat to 60°C)

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
10 mM 0.1543 mL 0.7714 mL 1.5428 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation
References
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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.

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Lercanidipine hydrochloride
Cat. No.:
HY-B0612A
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