Comparison

Donepezil HCl European Partner

Item no. S2462-100
Manufacturer Selleckchem
CASRN 120011-70-3
Amount 100 mg
Quantity options 10 mg 100 mg 1 g 200 mg 25 mg 50 mg
Category
Type Inhibitors
Specific against other
Smiles COC1=C(C=C2C(=C1)CC(C2=O)CC3CCN(CC3)CC4=CC=CC=C4)OC.Cl
ECLASS 10.1 32160490
ECLASS 11.0 32160490
UNSPSC 12000000
Alias bAChE,hAChE,AChR
Similar products Donepezil
Available
Storage Conditions
2 years -80 in solvent
Molecular Weight
416
Administration
Administered via i.p. or p.o.
Animal Models
Male Lister Hooded rats
Clinical Trials
Donepezil is currently being evaluated in Phase III clinical trials for Parkinson' s disease (PD) patients with dementia.
Dosages
18 uM/kg
Formulation
0.9% w:v NaCl (saline)
IC50
8.12 nM, 8.12 nM, 8.12 nM, 8.12 nM, 8.12 nM, 8.12 nM
In vitro
Donepezil inhibits the carbachol-stimulated increase in intracellular Ca2+ concentration in human SHSY5Y neuroblastoma cells in a concentration dependent manner, indicating that Donepezil have muscarinic antagonist activity. [2] A recent study shows that Donepezil can protect human umbilical vein endothelial cells (HUVECs) against H2O2-induced cell injury. This may be useful as a potential therapy for oxidative stress in cardiovascular and cerebrovascular diseases. [3]
In vivo
Intraperitoneal administration of Donepezil in rats produces a dose dependent increase in salivation and tremor, which are overt cholinergic behavioural signs, with an ED50 of 6 umol/kg. Donepezil is found to be somewhat less potent with a ED50 of 50 umol/kg following oral administration. [2]. When administered separately in vivo, 5-HT(4) receptor inducer, RS67333 (0.3 and 1 mg/kg) and Donepezil (1 mg/kg) improves recognition performances compared to saline treated mice, while co-administration of subactive doses of RS67333 (0.1mg/kg) and Donepezil (0.3 mg/kg) improves memory. However, this improvement is prevented if a 5-HT(4)R antagonist (GR125487, 10 mg/kg) is also administered. [4]
Kinase Assay
AChE inhibitory activity, PDGF receptor is immunoprecipitated from BALB/c 3T3 cell extracts with rabbit antiserum (for the murine PDGF receptor) for 2 hours on ice. Protein A-Sepharose beads are used to collect the antigen-antibody complexes. The immunoprecipitates are washed twice with TNET (50 mM Tris, pH 7.5, 140 mM NaCl, 5 mM EDTA, 1% Triton X-100), once with TNE (50 mM Tris, pH 7.5, 140 mM EDTA), and once with kinase buffer (20 mM Tris, pH 7.5, 10 mM MgCl2). After stimulation with PDGF (50 ng/ml) at 4 C for 10 minutes, different concentrations of the drug are added to the reaction mixture. PDGF receptor kinase activity is determined by incubation with 10 uCi [7-32P]-ATP and l uM ATP for 10 minutes at 4 C. Immune complexes are separated by SDS-PAGE on 7.5% gels.
Solubility (25C)
DMSO 1 mg/mL, Water 31 mg/mL, Ethanol 2 mg/mL
Information
Donepezil HCl is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM , respectively.This product is not soluble in PBS solution. Please do not dissolve it in PBS for administration.

Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.

All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.

Amount: 100 mg
Available: In stock
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