Lercanidipine
Based on 1 publication(s) in Google Scholar
Lercanidipine is a third-generation, lipophilic, brain-penetrant, vascular-selective and orally active dihydropyridine-calcium channel blocker with a pIC50 of 7.74 (converts from μM). Lercanidipine has long lasting antihypertensive action as well as reno- and neuro-protective effect. Lercanidipine also shows anti-oxidant, anti-inflammatory and anti-apoptotic properties. Lercanidipine can be used in cardiovascular and neurological research.
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- Pureza : 99.93%
- No. CAS: 100427-26-7
- Fòrmula: C36H41N3O6
- Peso molecular:611.73
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Lercanidipine
MoreVer todos los productos específicos de isoformas Calcium Channel
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Actividad biológica
Descripciòn
IC50 & Target
calcium channel[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LLC-MK2 | IC50 |
434.99 μM
Compound: Lercanidipine
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Cytotoxicity against rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay
Cytotoxicity against rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay
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[PMID: 20934347] |
| LLC-MK2 | IC50 |
8.43 μM
Compound: Lercanidipine
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Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi infected in rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay
Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi infected in rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay
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[PMID: 20934347] |
In Vitro
Lercanidipine (1, 10 μM, 24 h) exerts suppression of NO, ROS and TNF-a through down-regulation of iNOS, MMP-2/MMP-9, and HMGB1, as well as inhibition of MAPKs, Akt/IkB-a and NF-kB pathways in LPS/IFN-γ-induced VSMCs[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:LPS/IFN-γ-induced VSMC
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Concentration:1 and 10 μM
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Incubation Time:24 h
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Result:Down-regulated LPS/IFN-γ-induced iNOS, MMP-2/-9, NF-kB expression and IkB-a phosphorylation. Decreased cytosolic HMGB1 fraction and extracellular HMGB1 release while increasing nuclear HMGB1 fraction.
In Vivo
Lercanidipine (1.92-0.12 mg/kg, p.o., acute administration) lowers blood pressure effectively and dose-dependently in spontaneous hypertensive rats[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Albino male Wistar rats, middle cerebral artery occlusion (MCAo) model[3]
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Dosage:1, 0.5 and 0.25 mg/kg
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Administration:Intraperitoneal injection (i.p.), acute administration
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Result:Showed neuroprotective effect in focal cerebral ischemic-reperfusion injury model, most effective dose was found to be at 0.5 mg/kg.
Significantly attenuated percentage infarct volume, significantly improved the apparent diffusion coefficient.
Declined MMP-9 activity significantly in all Lercanidipine treated groups till 240 min post-reperfusion, while MMP-2 activity was inhibited only till 120 min post-reperfusion.
Decreased caspase-3 activity significantly in Lercanidipine 15 and 120 min post-reperfusion groups only. Exhibited significant reduction in caspase-9 activity in all groups except at 240 min post-reperfusion group.
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Animal Model:Male SHRs [4]
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Dosage:1.92, 0.96, 0.48, 0.24 and 0.12 mg/kg
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Administration:Oral gavage (p.o.), acute administration
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Result:Increased the AOC values of mean arterial pressure in a dose-dependent manner (285.4 mmHg×hour for 1.92 mg) as well as decreased BP.
Chemical Information
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No. CAS 100427-26-7
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Appearance Solid
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Peso molecular 611.73
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Fòrmula C36H41N3O6
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Color Light yellow to yellow
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SMILES
O=C(C1=C(C)NC(C)=C(C(OC)=O)C1C2=CC=CC([N+]([O-])=O)=C2)OC(C)(C)CN(CCC(C3=CC=CC=C3)C4=CC=CC=C4)C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Calcium
Mutations and clinical significance of calcium voltage-gated channel subunit alpha 1E (CACNA1E) in non-small cell lung cancer. [Abstract]2022 Mar:102:102527. PMID: 35026540
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (163.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
Protocolo
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Pureza y Documentación
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Ficha de datos (282 KB)
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SDS (557 KB)
- English - EN (557 KB)
- Français - FR (557 KB)
- Deutsch - DE (557 KB)
- Norwegian - NO (557 KB)
- Español - ES (557 KB)
- Swedish - SV (557 KB)
- Italian - IT (557 KB)
- Korean - KR (557 KB)
- Portuguese - PT (557 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Barrios, V., et al., Lercanidipine is an effective and well tolerated antihypertensive drug regardless the cardiovascular risk profile: The LAURA study. Int J Clin Pract, 2006. 60(11): p. 1364-70. [Content Brief]
[2]. Duda-Seiman D, et al. Calcium Channel Blockers--Benefits Upon Vascular Biology in Hypertensive Patients. Cardiovasc Hematol Agents Med Chem. 2015;13(1):54-62. [Content Brief]
[3]. Gupta S, et al. Neuroprotective effect of lercanidipine in middle cerebral artery occlusion model of stroke in rats. Exp Neurol. 2017 Feb;288:25-37. [Content Brief]
[4]. Yeh JL, et al. Lercanidipine and labedipinedilol--A attenuate lipopolysaccharide/interferon-γ-induced inflammation in rat vascular smooth muscle cells through inhibition of HMGB1 release and MMP-2, 9 activities. Atherosclerosis. 2013 Feb;226(2):364-72. [Content Brief]
[5]. Lee JJ, et al. Drug synergism of antihypertensive action in combination of telmisartan with lercanidipine in spontaneous hypertensive rats. Arch Pharm Res. 2010 Sep;33(9):1411-8. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6347 mL | 8.1735 mL | 16.3471 mL | 40.8677 mL |
| 5 mM | 0.3269 mL | 1.6347 mL | 3.2694 mL | 8.1735 mL | |
| 10 mM | 0.1635 mL | 0.8174 mL | 1.6347 mL | 4.0868 mL | |
| 15 mM | 0.1090 mL | 0.5449 mL | 1.0898 mL | 2.7245 mL | |
| 20 mM | 0.0817 mL | 0.4087 mL | 0.8174 mL | 2.0434 mL | |
| 25 mM | 0.0654 mL | 0.3269 mL | 0.6539 mL | 1.6347 mL | |
| 30 mM | 0.0545 mL | 0.2725 mL | 0.5449 mL | 1.3623 mL | |
| 40 mM | 0.0409 mL | 0.2043 mL | 0.4087 mL | 1.0217 mL | |
| 50 mM | 0.0327 mL | 0.1635 mL | 0.3269 mL | 0.8174 mL | |
| 60 mM | 0.0272 mL | 0.1362 mL | 0.2725 mL | 0.6811 mL | |
| 80 mM | 0.0204 mL | 0.1022 mL | 0.2043 mL | 0.5108 mL | |
| 100 mM | 0.0163 mL | 0.0817 mL | 0.1635 mL | 0.4087 mL |
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