Lacidipine

SKU: orb1227086

Description

Lacidipine (Lacipil, Motens) is a L-type calcium channel blocker.Lacidipine, a novel third-generation dihydropyridine calcium channel blocker, has been demonstrated effective for hypertension. lacidipine protects HKCs against apoptosis induced by ATP depl.(In Vitro):Lacidipine (0.01-100 μM; 24 h) inhibits HKCs proliferation in vitro in a concentration-dependent manner.Lacidipine (0.01-100 μM; 24 h) protects HKCs against apoptosis induced by ATP depletion and recovery by regulating the caspase-3 pathway.(In Vivo):Lacidipine (0.3, 1.0, 3.0 mg/kg; p.o.; single daily for 10 weeks) shows anti-atherogenic effects in the apoE-deficient mouse, and reduces plasma endothelin concentrations.

Key Properties

• CAS Number: 103890-78-4
• MW: 455.54
• Purity: >98% (HPLC)
• Formula: C₂₆H₃₃NO₆
• SMILES: O=C(C1=C(C)NC(C)=C(C(OCC)=O)C1C2=CC=CC=C2/C=C/C(OC(C)(C)C)=O)OCC
• Target: Calcium Channel
• Solubility: Ethanol: 22 mg/mL (48.29 mM); DMSO: 91 mg/mL (199.76 mM)

Bioactivity

• In Vivo:
  Lacidipine (0.3, 1.0, 3.0 mg/kg; p.o. ; single daily for 10 weeks) shows anti-atherogenic effects in the apoE-deficient mouse, and reduces plasma endothelin concentrations. Animal model: Female C57BL/6 mice (Homozygous; apoE-deficient; atherosclerosis model). Dosage: 0.3, 1.0, 3.0 mg/kg. Administration: Oral gavage; single daily for 10 weeks. Result: Induced a significant dose-dependent decrease in plasma endothelin levels. Significantly reduced the mean lesion area in a dose-related manner by 10, 17 and 53% for 0.3, 1.0, 3.0 mg/kg, respectively.
• In Vitro:
  Lacidipine (0.01-100 μM; 24 h) inhibits HKCs proliferation in vitro in a concentration-dependent manner. Lacidipine (0.01-100 μM; 24 h) protects HKCs against apoptosis induced by ATP depletion and recovery by regulating the caspase-3 pathway. Cell Proliferation Assay Cell line: HKC cells. Concentration: 0.01-100 μM Incubation time: 24 h. Result: Exhibited anti-proliferative activity in a concentration-dependent manner. Apoptosis Analysis Cell line: HKC cells (renal ischemia reperfusion (I/R) model). Concentration: 1, 10 μM. Incubation time: 24 h. Result: AA-induced HKC cells apoptosis, with proportion of early apoptotic cells of 1.47% and 0.30% for 1 and 10 μM dosage, respectively. Western blot analysis. Cell line: HKC cells (renal ischemia reperfusion (I/R) model). Concentration: 1, 10 μM. Incubation time: 24 h (pretreat). Result: Decreased the expression of cyt c of injured cells following ATP depletion and recovery. Significantly increased the expression of the Bcl-2 protein, but decreased the Bax protein.

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

Lacidipine | Lacipil | Lacimen | Motens | GR 43659 X

Quick Database Links

Gene Symbol

Calcium Channel