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MedKoo Cat#: 317635 | Name: Donepezil
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Donepezil is a medication used in the palliative treatment of Alzheimer's disease. Donepezil is used to improve cognition and behavior of people with Alzheimer's, but does not slow the progression of or cure the disease.

Chemical Structure

Donepezil
Donepezil
CAS#120014-06-4 (free base)

Theoretical Analysis

MedKoo Cat#: 317635

Name: Donepezil

CAS#: 120014-06-4 (free base)

Chemical Formula: C24H29NO3

Exact Mass: 379.2147

Molecular Weight: 379.49

Elemental Analysis: C, 75.96; H, 7.70; N, 3.69; O, 12.65

Price and Availability

Size Price Availability Quantity
1g USD 150.00 Ready to ship
2g USD 250.00 Ready to ship
5g USD 450.00 Ready to ship
10g USD 750.00 Ready to ship
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Related CAS #
120014-06-4 (free base) 120011-70-3 (HCl) 142698-19-9 (R-isomer) 142057-80-5 (S-isomer)
Synonym
HSDB 7743; HSDB7743; HSDB-7743; Donepezil
IUPAC/Chemical Name
2-((1-benzylpiperidin-4-yl)methyl)-5,6-dimethoxy-2,3-dihydro-1H-inden-1-one
InChi Key
ADEBPBSSDYVVLD-UHFFFAOYSA-N
InChi Code
InChI=1S/C24H29NO3/c1-27-22-14-19-13-20(24(26)21(19)15-23(22)28-2)12-17-8-10-25(11-9-17)16-18-6-4-3-5-7-18/h3-7,14-15,17,20H,8-13,16H2,1-2H3
SMILES Code
O=C1C(CC2CCN(CC3=CC=CC=C3)CC2)CC4=C1C=C(OC)C(OC)=C4
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Certificate of Analysis
View CoA: current batch, Lot#A24M07B10
Safety Data Sheet (SDS)
View Safety Data Sheet (SDS)
Instruction
View handling instruction
Biological target:
Donepezil (E2020 free base) is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bovine AChE and human AChE, respectively.
In vitro activity:
Donepezil (100 μM) decreased cell viability, but incubation with donepezil at concentrations of 0.1, 1, and 10 μM has no obvious effects on cell viability compared with control (Figure 1A). These results showed that pretreatment with donepezil at concentrations of 1 and 10 μM, compared to H2O2 group, significantly inhibits the H2O2‐induced reduction in cell viability (Figure 1B). It is demonstrated that lower concentrations of donepezil could protect H2O2‐induced HUVECs injury and may also have a similar protective effect on ischemic tissues. Reference: CNS Neurosci Ther. 2012 Feb;18(2):185-7. https://pubmed.ncbi.nlm.nih.gov/22313947/
In vivo activity:
The retrograde perfusion of the M(2)-M(4) receptor antagonist AFDX-384 (10 microM) induced a 500 and 300% increase in cortical and hippocampal acetylcholine release, in control and rivastigmine-treated rats, respectively, no increase in metrifonate-treated rats, and a 210% increase in donepezil-treated rats. In conclusion, chronic treatment of aging rats with metrifonate, rivastigmine and donepezil induces a long-lasting increase in acetylcholine levels, and reveals marked differences between the three drugs. Reference: J Neural Transm (Vienna). 2002 Jul;109(7-8):1067-80. https://pubmed.ncbi.nlm.nih.gov/12111444/
Solvent mg/mL mM
Solubility
DMSO 54.2 142.73
Water 2.0 5.27
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 379.49 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.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Kim HG, Moon M, Choi JG, Park G, Kim AJ, Hur J, Lee KT, Oh MS. Donepezil inhibits the amyloid-beta oligomer-induced microglial activation in vitro and in vivo. Neurotoxicology. 2014 Jan;40:23-32. doi: 10.1016/j.neuro.2013.10.004. Epub 2013 Nov 1. PMID: 24189446. 2. Huang ZH, Guo W, Zhang LL, Song SW, Hao CN, Duan JL. Donepezil protects endothelial cells against hydrogen peroxide-induced cell injury. CNS Neurosci Ther. 2012 Feb;18(2):185-7. doi: 10.1111/j.1755-5949.2011.00281.x. PMID: 22313947; PMCID: PMC6493582. 3. Miki A, Otori Y, Morimoto T, Okada M, Tano Y. Protective effect of donepezil on retinal ganglion cells in vitro and in vivo. Curr Eye Res. 2006 Jan;31(1):69-77. doi: 10.1080/02713680500477438. PMID: 16421021. 4. Scali C, Casamenti F, Bellucci A, Costagli C, Schmidt B, Pepeu G. Effect of subchronic administration of metrifonate, rivastigmine and donepezil on brain acetylcholine in aged F344 rats. J Neural Transm (Vienna). 2002 Jul;109(7-8):1067-80. doi: 10.1007/s007020200090. PMID: 12111444.
In vitro protocol:
1. Kim HG, Moon M, Choi JG, Park G, Kim AJ, Hur J, Lee KT, Oh MS. Donepezil inhibits the amyloid-beta oligomer-induced microglial activation in vitro and in vivo. Neurotoxicology. 2014 Jan;40:23-32. doi: 10.1016/j.neuro.2013.10.004. Epub 2013 Nov 1. PMID: 24189446. 2. Huang ZH, Guo W, Zhang LL, Song SW, Hao CN, Duan JL. Donepezil protects endothelial cells against hydrogen peroxide-induced cell injury. CNS Neurosci Ther. 2012 Feb;18(2):185-7. doi: 10.1111/j.1755-5949.2011.00281.x. PMID: 22313947; PMCID: PMC6493582.
In vivo protocol:
1. Miki A, Otori Y, Morimoto T, Okada M, Tano Y. Protective effect of donepezil on retinal ganglion cells in vitro and in vivo. Curr Eye Res. 2006 Jan;31(1):69-77. doi: 10.1080/02713680500477438. PMID: 16421021. 2. Scali C, Casamenti F, Bellucci A, Costagli C, Schmidt B, Pepeu G. Effect of subchronic administration of metrifonate, rivastigmine and donepezil on brain acetylcholine in aged F344 rats. J Neural Transm (Vienna). 2002 Jul;109(7-8):1067-80. doi: 10.1007/s007020200090. PMID: 12111444.
1: Cummings J, Lai TJ, Hemrungrojn S, Mohandas E, Yun Kim S, Nair G, Dash A. Role of Donepezil in the Management of Neuropsychiatric Symptoms in Alzheimer's Disease and Dementia with Lewy Bodies. CNS Neurosci Ther. 2016 Mar;22(3):159-66. doi: 10.1111/cns.12484. Epub 2016 Jan 18. Review. PubMed PMID: 26778658. 2: Ismaili L, Refouvelet B, Benchekroun M, Brogi S, Brindisi M, Gemma S, Campiani G, Filipic S, Agbaba D, Esteban G, Unzeta M, Nikolic K, Butini S, Marco-Contelles J. Multitarget compounds bearing tacrine- and donepezil-like structural and functional motifs for the potential treatment of Alzheimer's disease. Prog Neurobiol. 2016 Jan 18. pii: S0301-0082(15)00162-8. doi: 10.1016/j.pneurobio.2015.12.003. [Epub ahead of print] Review. PubMed PMID: 26797191. 3: Szigeti K, Hafeez MU. Exploring the role of donepezil in dementia with Lewy bodies. Drugs Today (Barc). 2015 Oct;51(10):579-90. doi: 10.1358/dot.2015.51.10.2389166. Review. PubMed PMID: 26583300. 4: Lee JH, Jeong SK, Kim BC, Park KW, Dash A. Donepezil across the spectrum of Alzheimer's disease: dose optimization and clinical relevance. Acta Neurol Scand. 2015 May;131(5):259-67. doi: 10.1111/ane.12386. Epub 2015 Feb 18. Review. PubMed PMID: 25690270. 5: Lane RM, Darreh-Shori T. Understanding the beneficial and detrimental effects of donepezil and rivastigmine to improve their therapeutic value. J Alzheimers Dis. 2015;44(4):1039-62. doi: 10.3233/JAD-142268. Review. PubMed PMID: 25408210. 6: de Medeiros K, Basting A. "Shall I compare thee to a dose of donepezil?": cultural arts interventions in dementia care research. Gerontologist. 2014 Jun;54(3):344-53. doi: 10.1093/geront/gnt055. Epub 2013 Jun 7. Review. PubMed PMID: 23749388. 7: Prvulovic D, Schneider B. Pharmacokinetic and pharmacodynamic evaluation of donepezil for the treatment of Alzheimer's disease. Expert Opin Drug Metab Toxicol. 2014 Jul;10(7):1039-50. doi: 10.1517/17425255.2014.915028. Epub 2014 Apr 30. Review. PubMed PMID: 24785550. 8: Rodrigues Simões MC, Dias Viegas FP, Moreira MS, de Freitas Silva M, Riquiel MM, da Rosa PM, Castelli MR, dos Santos MH, Soares MG, Viegas C Jr. Donepezil: an important prototype to the design of new drug candidates for Alzheimer's disease. Mini Rev Med Chem. 2014 Jan;14(1):2-19. Review. PubMed PMID: 24251806. 9: Ikeda K, Yanagihashi M, Sawada M, Hanashiro S, Kawabe K, Iwasaki Y. Donepezil-induced cervical dystonia in Alzheimer's disease: a case report and literature review of dystonia due to cholinesterase inhibitors. Intern Med. 2014;53(9):1007-10. Epub 2014 May 1. Review. PubMed PMID: 24785894. 10: Tan CC, Yu JT, Wang HF, Tan MS, Meng XF, Wang C, Jiang T, Zhu XC, Tan L. Efficacy and safety of donepezil, galantamine, rivastigmine, and memantine for the treatment of Alzheimer's disease: a systematic review and meta-analysis. J Alzheimers Dis. 2014;41(2):615-31. doi: 10.3233/JAD-132690. Review. PubMed PMID: 24662102. 11: Cummings JL, Geldmacher D, Farlow M, Sabbagh M, Christensen D, Betz P. High-dose donepezil (23 mg/day) for the treatment of moderate and severe Alzheimer's disease: drug profile and clinical guidelines. CNS Neurosci Ther. 2013 May;19(5):294-301. doi: 10.1111/cns.12076. Epub 2013 Mar 6. Review. PubMed PMID: 23462265. 12: Toda N. [Nitrergic cerebrovascular regulation as affected by donepezil]. Nihon Yakurigaku Zasshi. 2013 Mar;141(3):150-4. Review. Japanese. PubMed PMID: 23470480. 13: Molino I, Colucci L, Fasanaro AM, Traini E, Amenta F. Efficacy of memantine, donepezil, or their association in moderate-severe Alzheimer's disease: a review of clinical trials. ScientificWorldJournal. 2013 Oct 29;2013:925702. doi: 10.1155/2013/925702. eCollection 2013. Review. PubMed PMID: 24288512; PubMed Central PMCID: PMC3830825. 14: Cheewakriengkrai L, Gauthier S. A 10-year perspective on donepezil. Expert Opin Pharmacother. 2013 Feb;14(3):331-8. doi: 10.1517/14656566.2013.760543. Epub 2013 Jan 14. Review. PubMed PMID: 23316713. 15: Thakurathi N, Vincenzi B, Henderson DC. Assessing the prospect of donepezil in improving cognitive impairment in patients with schizophrenia. Expert Opin Investig Drugs. 2013 Feb;22(2):259-65. doi: 10.1517/13543784.2013.750650. Epub 2012 Dec 9. Review. PubMed PMID: 23215841. 16: Damulin IV. [Donepezil in Alzheimer's disease and vascular dementia]. Zh Nevrol Psikhiatr Im S S Korsakova. 2013;113(7):71-5. Review. Russian. PubMed PMID: 24073452. 17: Di Santo SG, Prinelli F, Adorni F, Caltagirone C, Musicco M. A meta-analysis of the efficacy of donepezil, rivastigmine, galantamine, and memantine in relation to severity of Alzheimer's disease. J Alzheimers Dis. 2013;35(2):349-61. doi: 10.3233/JAD-122140. Review. PubMed PMID: 23411693. 18: Constantinescu MI, Constantinescu DP, Andercou A, Mironiuc IA. Influence of sildenafil and donepezil administration on the serum redox balance in experimentally induced lower limb critical ischemia. Clujul Med. 2013;86(3):250-8. Epub 2013 Aug 5. Review. PubMed PMID: 26527957; PubMed Central PMCID: PMC4462506. 19: Christensen DD. Higher-dose (23 mg/day) donepezil formulation for the treatment of patients with moderate-to-severe Alzheimer's disease. Postgrad Med. 2012 Nov;124(6):110-6. doi: 10.3810/pgm.2012.11.2589. Review. PubMed PMID: 23322144. 20: Doody RS, Cummings JL, Farlow MR. Reviewing the role of donepezil in the treatment of Alzheimer's disease. Curr Alzheimer Res. 2012 Sep;9(7):773-81. Review. PubMed PMID: 22175653.