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Donepezil Hydrochloride

Catalog No. T6478   CAS 120011-70-3
Synonyms: Aricept, BNAG, E2020, Donepezil HCl

Donepezil HCl(Aricept) is a selective and effective AChE inhibitor for bAChE and hAChE (IC50: 8.12/11.6 nM).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Donepezil Hydrochloride Chemical Structure
Donepezil Hydrochloride, CAS 120011-70-3
Pack Size Availability Price/USD Quantity
25 mg In stock $ 44.00
50 mg In stock $ 63.00
100 mg In stock $ 85.00
200 mg In stock $ 129.00
500 mg In stock $ 216.00
1 mL * 10 mM (in DMSO) In stock $ 68.00
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Purity: 99.89%
Purity: 99.8%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Donepezil HCl(Aricept) is a selective and effective AChE inhibitor for bAChE and hAChE (IC50: 8.12/11.6 nM).
Targets&IC50 AChE (human):11.6 nM, AChE (bovine):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 Water2-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 μmol/kg. Donepezil is found to be somewhat less potent with a ED50 of 50 μmol/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 (0.1 mg/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 [3H]-Pyrilamine binding to histamine (H1) receptors in guinea pig cerebellum membranes.: Antagonists are incubated with guinea pig cerebellum membranes (0.6 mg/ml) and [3H]-pyrilamine (1.2 nM) in 0.5 ml 50 mM PBS, pH 7.5, for 30 min at 25 ℃. The incubation is ended by the addition of 5 ml of ice-cold PBS containing 2 μM pyrilamine and the collection of membranes on Whatman GF/B filters. Then the filters are washed with 3 × 5 ml of ice-cold PBS plus 2 μM pyrilamine and transferred to counting vials. The radioactivity retained by each filter is measured by liquid scintillation counting in 3 ml of HiSafe 3. Specific binding is determined from the difference between the [3H]-pyrilamine bound in the absence and in the presence of a large molar excess (10 μM) of unlabeled promethazine.
Synonyms Aricept, BNAG, E2020, Donepezil HCl
Molecular Weight 415.96
Formula C24H29NO3·HCl
CAS No. 120011-70-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 4.2 mg/mL (10 mM)

H2O: 31.2 mg/mL (75 mM)

TargetMolReferences and Literature

1. Ogura H, et al. Methods Find Exp Clin Pharmacol. 2000, 22(8), 609-613. 2. Snape MF, et al. Neuropharmacology. 1999, 38(1), 181-193. 3. Huang ZH, et al. CNS Neurosci Ther. 2012, 18(2), 185-187. 4. Freret T, et al. Behav Brain Res. 2012 https://dx.doi.org/10.1016/j.bbr.2012.02.012.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Approved Drug Library Anti-Neurodegenerative Disease Compound Library Anti-Cancer Drug Library EMA Approved Drug Library Anti-Cancer Clinical Compound Library Membrane Protein-targeted Compound Library Inhibitor Library Drug Repurposing Compound Library Bioactive Compounds Library Max CNS-Penetrant Compound Library

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Keywords

Donepezil Hydrochloride 120011-70-3 Neuroscience AChE AChR Donepezil E 2020 amyloid-β E-2020 Aricept inhibit Cholinesterase (ChE) BNAG E2020 Donepezil HCl Neuroprotective Inhibitor inhibitor

 

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