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Donepezil HCl Europäischer Partner

ArtNr S2462-50
Hersteller Selleckchem
CAS-Nr. 120011-70-3
Menge 50 mg
Quantity options 10 mg 100 mg 1 g 200 mg 25 mg 50 mg
Kategorie
Typ 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
Lieferbar
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.

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Alle Produkte sind nur für Forschungszwecke bestimmt. Nicht für den menschlichen, tierärztlichen oder therapeutischen Gebrauch.

Menge: 50 mg
Lieferbar: In stock
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