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Lercanidipine hydrochloride

Catalog No. T6874 CAS 132866-11-6

Synonyms: Corifeo, Carmen, Cardiovasc

Lercanidipine hydrochloride (Corifeo) is a calcium channel blocker of the dihydropyridine class.

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Lercanidipine hydrochloride Chemical Structure

Lercanidipine hydrochloride, CAS 132866-11-6

Pack Size	Availability	Price/USD
10 mg	In stock	$ 45.00
25 mg	In stock	$ 90.00
50 mg	In stock	$ 170.00
100 mg	In stock	$ 266.00
200 mg	In stock	$ 339.00
1 mL * 10 mM (in DMSO)	In stock	$ 48.00

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Purity: 100%

Purity: 99.81%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Lercanidipine hydrochloride (Corifeo) is a calcium channel blocker of the dihydropyridine class.
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].
Kinase Assay	Cell-free enzyme assays are performed to determine the selective inhibition of ROCK1 and ROCK2 by SLx-2119. Reactions are performed on non-binding surface microplates. Four mU of human ROCK1 and ROCK2 are used to phosphorylate 30 μM of the synthetic ROCK peptide substrate S6 Long, prepared at American Peptide with the addition of 10 μM ATP, containing?33P-ATP in the presence of 10 mM Mg2+, 50 mM Tris, pH 7.5, 0.1 mM EGTA and 1 mM DTT at room temperature. One unit is the amount of kinase needed to catalyze the transfer of 1 nmol phosphate/min to the peptide. The reactions are allowed to proceed for 45 minutes and then stopped with 3% phosphoric acid to a final concentration of 1%. The reactions are captured on phospho cellulose filtration microplates and washed with 75 mM phosphoric acid and methanol using a vacuum manifold. Phosphorylation is measured on a Perkin-Elmer MicroBeta 1450.
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)

Synonyms	Corifeo, Carmen, Cardiovasc
Molecular Weight	648.19
Formula	C36H41N3O6·HCl
CAS No.	132866-11-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 64.8 mg/mL (100 mM)

Ethanol: 6.5 mg/mL (10 mM)

References and Literature

1. Shereen M. Tawakkol, et al. Analytical Chemistry Letters. 2014, 4:255-266. 2. Canavesi M, et al. J Cardiovasc Pharmacol. 2004, 44(4):416-422. 3. Gasser R, et al. Journal of Clinical and Basic Cardiology. 1999, 2(2):169-174. 4. Epstein M, et al. Heart Dis. 2001, 3(6):398-407. 5. Selvaraj N, et al. J Clin Diagn Res. 2015, 9(11):FF01-5.

Citations

1. Guo Z, Tian E, Chen S, et al.Lercanidipine’s Antioxidative Effect Prevents Noise-Induced Hearing Loss.Antioxidants.2024, 13(3): 327.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Calcium Channel Compound Library Anti-Hypertension Compound Library Neuronal Signaling Compound Library Approved Drug Library Anti-COVID-19 Compound Library Ion Channel Inhibitor Library Metabolism Compound Library

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Keywords

Lercanidipine hydrochloride 132866-11-6 Membrane transporter/Ion channel Metabolism Calcium Channel Corifeo antihypertensive Inhibitor calcium Lercanidipine Lercanidipine Hydrochloride Carmen reno-protective Ca2+ channels Cardiovasc Ca channels channel inhibit inhibitor

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