Lercanidipine hydrochloride

SKU: orb1300387

Description

Lercanidipine hydrochloride is a dihydropyridine calcium channel blocker used in research to study hypertension and vascular smooth muscle function. It is applied in both in vitro assays and in vivo models to investigate its mechanisms of action and hemodynamic effects.

Research Area

Cell Biology, Immunology & Inflammation, Metabolism Research, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 132866-11-6
• MW: 648.19
• Purity: >99.99% (May vary between batches)
• Formula: C₃₆H₄₁N₃O₆·HCl
• SMILES: Cl.COC(=O)C1=C(C)NC(C)=C(C1c1cccc(c1)[N+]([O-])=O)C(=O)OC(C)(C)CN(C)CCC(c1ccccc1)c1ccccc1
• Target: NF-κB,Apoptosis,ROS,Reactive Oxygen Species,Calcium Channel,p38 MAPK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.09 mM);DMSO:50 mg/mL (77.14 mM);Ethanol:6.5 mg/mL (10.03 mM)

Bioactivity

• In Vivo:
  In chronically catheterised dogs with experimental renovascular hypertension, lercanidipine decreases diastolic blood pressure in a dose-dependent manner (ED25 = 0.9 mg/kg p.o). In the same animals, long term application of lercanidipine showed permanent decrease of diastolic blood pressure indicating no tolerance of the antihypertensive effect. Lercanidipine possesses significant anticonvulsant effect. It does not affect the muscle coordination or locomotor activity in mice. In clinical studies, lercanidipine has a 24-hour antihypertensive effect and causes no significant increase in heart rate. Lercanidipine has been shown to be effective in a wide range of hypertensive patients, including mild-to-moderate hypertension, severe hypertension, the elderly, and those with isolated systolic hypertension. It is associated with a low rate of adverse events.
• In Vitro:
  In vitro calcium antagonistic activity of Lercanidipine is clearly related to a gradual block of calcium entry into smooth muscle cells via L-type calcium channels. lercanidipine inhibits cellular cholesteryl ester formation. At concentrations similar to those occurring in clinical practice, it may inhibit in vitro macrophage functions involved in atherogenesis and plaque stability.
• Cell Research:
  Cells are incubated for 24 hours in DMEM+EFAF 0.2% and lercanidipine, then with lercanidipine and AcLDL for 24 hours. In the last 2 hours [14C]-oleic acid albumin complex is added for the determination of cholesterol esterification (ACAT activity). (Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

channel, CalciumChannel, Corifeo, antihypertensive, Ca channels, Ca2+ channels, calcium, Calcium Channel, Carmen, Cardiovasc, Inhibitor, Lercanidipine, Lercanidipine Hydrochloride, Lercanidipine hydrochloride, inhibit, reno-protective

Compound Identifiers

PubChem CID

157917