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Postion:Product Catalog >API>Nervous system drugs>Drug Metabolism in Human Brain>Donepezil
Donepezil
  • Donepezil

Donepezil NEW

Price $31 $50 $70
Package 5mg 10mg 25mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-19

Product Details

Product Name: Donepezil CAS No.: 120014-06-4
Purity: 99.8% Supply Ability: 10g
Release date: 2024/11/19

Product Introduction

Bioactivity

NameDonepezil
DescriptionDonepezil (Aricept) is a piperidine-based, potent, specific, and reversible inhibitor of acetylcholinesterase (AChE). It can be used for the treatment of mild to moderate dementia of the Alzheimer's type.
Cell ResearchCell lines: retinal ganglion cells (RGCs). Concentrations: 0.1-10 μM. Incubation Time: 3 days. RGC survival after exposure to each reagent (glutamate, donepezil, tacrine, galanthamine, and HA14-1) is measured by calcein-AM staining after 3 days in culture, Briefly, cells are incubated in 1 μM calcein-AM in PBS for 15 minutes at 37℃. After the medium is replaced with fresh PBS, cells are examined under a fluorescence microscope using a fluorescein filter. The total number of surviving RGCs defined as cells with a calcein-AM stained cell body and a process extending at least two cell diameters from the cell body is counted in each well. The number of surviving RGCs without any drug served as a control.
Animal ResearchAnimal Models: male C57BL/6 wild-type and CGRP(?/?) mice (10-12 weeks old, 21–24 g). Formulation: added to the food powder. Dosages: 1.5 mg/kg (i.g.)
In vitroDonepezil has 500-1000-fold more selective for AChE over butyrylcholinesterase (BuChE). Short- and long-exposure of SH-SY5Y human neuroblastoma cells to donepezil induces a concentration-dependent inhibition of cell proliferation unrelated to muscarinic or nicotinic receptor blockade or apoptosis. Donepezil reduces the number of cells in the S-G2/M phases of the cell cycle, increases the G0/G1 population, and reduces the expression of two cyclins of the G1/S and G2/M transitions, cyclin E and cyclin B, in parallel with an increase in the expression of the cell cycle inhibitor p21. In addition, donepezil increases action potential-dependent dopamine release and modulates nicotinic receptors of substantia nigra dopaminergic neurons[1].
In vivoIn plasma, urine, and bile, most donepezil metabolites are O-glucuronides. After oral ingestion, peak plasma concentrations are achieved in 3-5 hours and its absorption is not affected by food. Donepezil is slowly absorbed from the gastrointestinal tract and has a terminal elimination half-life of 50-70 hours in young volunteers (>100 hours in elderly subjects). After extensive metabolization in the liver, the parent compound is 93% bound to plasma proteins. Donepezil is metabolized in the liver via the cytochrome P450 system (CYP1A2-, CYP2D6-, CYP3A4-related enzymes). In animals, donepezil is found unchanged in the brain, and no metabolites are detected in the nervous tissue. Donepezil has linear pharmacokinetics over a dose range of 1-10 mg/day. 96% of circulating donepezil is protein bound [1].
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationDMSO : 50 mg/mL (131.75 mM)
KeywordsAChE | Donepezil | Cholinesterase (ChE) | Inhibitor | inhibit | hAChE | E 2020 | E-2020 | bAChE
Inhibitors Related1-Naphthyl acetate | DL-Menthol | Ethyl (triphenylphosphoranylidene) acetate | 4-Methylbenzylidene camphor | Isoeugenol acetate | Diethyltoluamide | Nizatidine | Methyl tridecanoate | Trimethylammonium chloride | Trimyristin
Related Compound LibrariesBioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Neuronal Signaling Compound Library | Drug-induced Liver Injury (DILI) Compound Library | Drug Repurposing Compound Library | Inhibitor Library | NO PAINS Compound Library | FDA-Approved Drug Library | Orally Active Compound Library | Bioactive Compounds Library Max

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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