Home Transmembrane Transporters Calcium Channel inhibitor Lercanidipine hydrochloride

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Lercanidipine hydrochloride Calcium Channel inhibitor

Cat.No.S4597

Lercanidipine is a calcium channel blocker of the dihydropyridine class.
Lercanidipine hydrochloride Calcium Channel inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 648.19

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Quality Control

Batch: Purity: 99.98%
99.98

Solubility

In vitro
Batch:

DMSO : 66 mg/mL (101.82 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 1 mg/mL

Water : Insoluble

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In vivo
Batch:

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 648.19 Formula

C36H41N3O6.HCl

 Storage (From the date of receipt)
CAS No. 132866-11-6 Download SDF Storage of Stock Solutions

Mechanism of Action

Targets/IC50/Ki
Calcium channel
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.
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.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/11975824/
  • [5] https://pubmed.ncbi.nlm.nih.gov/26673531/

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