Lercanidipine hydrochloride

Catalog No.S4597

For research use only.

Lercanidipine is a calcium channel blocker of the dihydropyridine class.

Lercanidipine hydrochloride Chemical Structure

CAS No. 132866-11-6

Selleck's Lercanidipine hydrochloride has been cited by 1 Publication

Purity & Quality Control

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Biological Activity

Description Lercanidipine is a calcium channel blocker of the dihydropyridine class.
Targets
Calcium channel [1]
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[1].

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[3]. Lercanidipine possesses significant anticonvulsant effect. It does not affect the muscle coordination or locomotor activity in mice[5]. 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[4].

Protocol (from reference)

Cell Research:

[2]

  • Cell lines: Mouse peritoneal macrophages
  • Concentrations: 0.1, 1, 5, 10, 15 μM
  • Incubation Time: 48 h
  • Method:

    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).

Animal Research:

[5]

  • Animal Models: Adult male Swiss albino mice
  • Dosages: 1 and 3 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 648.19
Formula

C36H41N3O6.HCl

CAS No. 132866-11-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C(C(=C(N1)C)C(=O)OC(C)(C)CN(C)CCC(C2=CC=CC=C2)C3=CC=CC=C3)C4=CC(=CC=C4)[N+](=O)[O-])C(=O)OC.Cl

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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