Lacidipine

SKU: orb1308604

Description

Lacidipine

Research Area

Cell Biology, Immunology & Inflammation, Metabolism Research, Pharmacology & Drug Discovery, Protein Biochemistry, Signal Transduction

Key Properties

• CAS Number: 103890-78-4
• MW: 455.54
• Purity: 99.98%
• Formula: C₂₆H₃₃NO₆
• SMILES: C(OCC)(=O)C=1C(C(C(OCC)=O)=C(C)NC1C)C2=C(/C=C/C(OC(C)(C)C)=O)C=CC=C2
• Target: Apoptosis,Caspase,Reactive Oxygen Species,Calcium Channel
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.24 mM);Ethanol:21 mg/mL (46.1 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:84 mg/mL (184.4 mM)

Bioactivity

• In Vivo:
  Lacidipine has non-significant effects on blood pressure but inhibit the paradoxical increases in plasma renin activity (PRA) and in renin mRNA in kidney that are found in salt-loaded stroke-prone spontaneously hypertensive rats (SHRSP). Lacidipine restore the physiological downregulation of renin production by high salt and reduces left ventricular hypertrophy and mRNA levels of atrial natriuretic factor and transforming growth factor-beta1. Lacidipine (1 and 3 mg/kg) also effectively increases calcium concentration significantly in ovariectomized rats. Lacidipine, a dihydropyridine-type calcium antagonist, reduce the cardiac hypertrophy an the cardiacendothelin-1 (ET-1) gene overexpression occurring in salt-loaded stroke-prone spontaneously hypertensive rats (SL-SHRSP), an effect occurring without systolic blood pressure (SBP) change. Lacidipine exerts a dose-related Inhibition of ventricle hypertrophy and preproET-1 mRNA expression in SHRSP and indicate that this effect is unrelated to SBP changes.
• In Vitro:
  Lacidipine, an L-type Ca(2+) channel blocker that also inhibits [Ca(2+)](ER) efflux, enhances folding, trafficking, and activity of degradation-prone glucocerebrosidase (GC) variants. Lacidipine remodels mutated GC proteostasis by simultaneously activating a series of distinct molecular mechanisms, namely modulation of Ca(2+) homeostasis, upregulation o the ER chaperone BiP, and moderate induction o the unfolded protein response. Lacidipine almost completely inhibits cholesterol esterification in cholesterol loaded mouse cultured peritoneal macrophages.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

inhibit, hypertension, GX 1048, GX1048, GX-1048, GR-43659X, Inhibitor, HKC cells, Lacidipine, CalciumChannel, Apoptosis, atherosclerosis, Caspase, Ca channels, Ca2+ channels, Calcium Channel, AKI, SN 305, SN305, SN-305, Reactive Oxygen Species, ReactiveOxygenSpecies

Compound Identifiers

PubChem CID

5311217