Lercanidipine hydrochloride

SKU: orb1222750

Description

Lercanidipine hydrochloride is a calcium channel blocker used in the treatment of hypertension.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 132866-11-6
• MW: 648.19
• Purity: >98% (HPLC)
• Formula: C₃₆H₄₁N₃O₆·HCl
• SMILES: CC1=C(C(C(=C(N1)C)C(=O)OC(C)(C)CN(C)CCC(c1ccccc1)c1ccccc1)c1cc(ccc1)[N+](=O)[O-])C(=O)OC.Cl
• Target: AChR
• Solubility: DMSO : 50 mg/mL 77.14 mM; H2O : < 0.1 mg/mL

Bioactivity

• In Vivo:
  Animal model: Albino male Wistar rats, middle cerebral artery occlusion (MCAo) model. Dosage: 1, 0.5 and 0.25 mg/kg. Administration: Intraperitoneal injection (i.p.), acute administration. 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. Animal model: Male SHRs. Dosage: 1.92, 0.96, 0.48, 0.24 and 0.12 mg/kg. Administration: Oral gavage (p.o.) for once. 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.
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• In Vitro:
  Western blot analysis. Cell line: LPS/IFN-γ-induced VSMC. Concentration: 1 and 10 μM. Incubation time: 24 h. 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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Lercanidipine hydrochloride | Renovia | Vasodip | R 75

Quick Database Links

Gene Symbol

AChR