Donepezil hydrochloride

Pricing Availability   Qty
Description: Potent AChE inhibitor
Alternative Names: E 2020
Chemical Name: 2,3-Dihydro-5,6-dimethoxy-2-[[1-(phenylmethyl)-4-piperidinyl]methyl]-1H-inden-1-one hydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations (3)
Reviews
Literature (1)

Biological Activity for Donepezil hydrochloride

Donepezil hydrochloride is a potent and selective acetylcholinesterase inhibitor (IC50 = 5.7 nM). In animal models of Alzheimer's disease, Donepezil reduces brain tissue Aβ protein and plaque deposition, restores normal glucose metabolism, reduces neuroinflammation and rescues cognitive dysfunction and memory deficits. The pro-cognitive effects are potentiated by combination with Mefloquine (Cat. No. 6819). In vitro Donepezil reduces LPS-induced inflammation and protects against mitochondrial membrane potential damage.

Technical Data for Donepezil hydrochloride

M. Wt 415.95
Formula C24H29NO3.HCl
Storage Desiccate at RT
Purity ≥99% (HPLC)
CAS Number 120011-70-3
PubChem ID 5741
InChI Key XWAIAVWHZJNZQQ-UHFFFAOYSA-N
Smiles O=C2C(CC3CCN(CC4=CC=CC=C4)CC3)CC1=CC(OC)=C(OC)C=C12.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Donepezil hydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 20.8 50

Preparing Stock Solutions for Donepezil hydrochloride

The following data is based on the product molecular weight 415.95. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 4.81 mL 24.04 mL 48.08 mL
2.5 mM 0.96 mL 4.81 mL 9.62 mL
5 mM 0.48 mL 2.4 mL 4.81 mL
25 mM 0.1 mL 0.48 mL 0.96 mL

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Product Datasheets for Donepezil hydrochloride

Certificate of Analysis / Product Datasheet
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References for Donepezil hydrochloride

References are publications that support the biological activity of the product.

Sugimoto et al (1995) Synthesis and structure-activity relationships of acetylcholinesterase inhibitors: 1-benzyl-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine hydrochloride and related compounds. J.Med.Chem. 38 4821 PMID: 7490731

Kryger et al (1999) Structure of acetylcholinesterase complexed with E2020 (Aricept): implications for the design of new anti-Alzheimer drugs. Structure 7 297 PMID: 10368299

Sugimoto et al (2000) Donepezil hydrochloride (E2020) and other acetylcholinesterase inhibitors. Curr.Med.Chem. 7 303 PMID: 10637367

Romberg et al (2011) Impaired attention in the 3xTgAD mouse model of Alzheimer's disease: rescue by donepezil (Aricept). J.Neurosci. 31 3500 PMID: 21368062

Droguerre et al (2020) Efficacy of THN201, a combination of donepezil and mefloquine, to reverse neurocognitive deficits in Alzheimer's disease. Front.Neurosci. 14 PMID: 32612499

Hugon et al (2022) Impact of donepezil on brain glucose metabolism assessed using [18F]2-fluoro-2-deoxy-D-glucose positron emission tomography imaging in a mouse model of Alzheimer's disease induced by intracerebroventricular injection of amyloid-beta peptid Front.Neurosci. 16 PMID: 35281502

Kim et al (2021) Donepezil regulates LPS and Aβ-stimulated neuroinflammation through MAPK/NLRP3 inflammasome/STAT3 signaling. Int.J.Mol.Sci. 22 10637 PMID: 34638977


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Keywords: Donepezil hydrochloride, Donepezil hydrochloride supplier, acetylcholinesterase, ache, selective, potent, inhibitors, inhibits, E2020, neurodegeneration, alzheimers, amyloid, beta, AB, neuroinflammation, Aβ, E, 2020, Cholinesterases, 4385, Tocris Bioscience

3 Citations for Donepezil hydrochloride

Citations are publications that use Tocris products. Selected citations for Donepezil hydrochloride include:

Rennekamp et al (2016) σ1 receptor ligands control a switch between passive and active threat responses. Nat Chem Biol 12 552 PMID: 27239788

Morris et al (2015) Network dysfunction in α-synuclein transgenic mice and human Lewy body dementia. Ann Clin Transl Neurol 2 1012 PMID: 26732627

Mercedes et al (2017) The proof-of-concept of ASS234: Peripherally administered ASS234 enters the central nervous system and reduces pathology in a male mouse model of Alzheimer disease. J Psychiatry Neurosci 42 59-69 PMID: 27636528


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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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Alzheimer's Disease Poster

Alzheimer's Disease Poster

Alzheimer's disease (AD) is a debilitating and progressive neurodegenerative disease and the most common cause of dementia, affecting approximately 30% of individuals aged over 85 years. This poster summarizes the cellular and molecular mechanisms of AD.