Lercanidipine hydrochloride

Catalog No.S4597 Batch:S459702

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Technical Data

Formula

C36H41N3O6.HCl
Molecular Weight 648.19 CAS No. 132866-11-6
Solubility (25°C)* In vitro DMSO 66 mg/mL (101.82 mM)
Ethanol 1 mg/mL (1.54 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 Assay:

[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 Study:

[5]
  • Animal Models

    Adult male Swiss albino mice

  • Dosages

    1 and 3 mg/kg

  • Administration

    i.p.

Selleck's Lercanidipine hydrochloride has been cited by 1 publication

Structure-dependent complexation of Fe3+ by anthracyclines. 2. The roles of methoxy and daunosamine functionalities [Nawara K, et al. J Phys Chem B, 2013, 117(23):6868-73] PubMed: 23692121

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.