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[1][2][3][4][5].

Product Specifications

CAS Number

[100427-26-7]

UNSPSC

12352005

Hazard Statement

H315-H319-H320

Target

Apoptosis; Calcium Channel; NF-κB; p38 MAPK; Reactive Oxygen Species (ROS)

Type

Reference compound

Related Pathways

Apoptosis; Immunology/Inflammation; MAPK/ERK Pathway; Membrane Transporter/Ion Channel; Metabolic Enzyme/Protease; Neuronal Signaling; NF-κB

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/Lercanidipine.html

Purity

99.65

Solubility

DMSO : 100 mg/mL (ultrasonic)

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

Molecular Formula

C36H41N3O6

Molecular Weight

611.73

Precautions

P264-P280-P302+P352-P305+P351+P338-P362

References & Citations

[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.|[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.|[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.|[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.|[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.