Lercanidipine hydrochloride

Catalog No.S4597

Lercanidipine hydrochloride Chemical Structure

Molecular Weight(MW): 648.19

Lercanidipine is a calcium channel blocker of the dihydropyridine class.

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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

Cell Research:

[2]

+ Expand
  • 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).


    (Only for Reference)
Animal Research:

[5]

+ Expand
  • Animal Models: Adult male Swiss albino mice
  • Formulation: Distilled water 
  • Dosages: 1 and 3 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 66 mg/mL (101.82 mM)
Ethanol 1 mg/mL (1.54 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 648.19
Formula

C36H41N3O6.HCl

CAS No. 132866-11-6
Storage powder
in solvent
Synonyms

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID