| Donepezil HClAChE inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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- Purity = 98.32%
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Chemical structure
| Cell experiment [1,2]: | |
Cell lines | Human SHSY5Y neuroblastoma cells, human umbilical vein endothelial cells |
Preparation method | Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition | 1 h |
Applications | Donepezil dose-dependently inhibited the carbachol-stimulated increase in intracellular Ca2+ concentration in human SHSY5Y neuroblastoma cells with the IC50 of 4.0 ± 0.2 μM. Donepezil protected human umbilical vein endothelial cells (HUVECs) against H2O2-induced cell injury. Donepezil (100 μM) decreased cell viability. Pretreatment with donepezil at concentrations of 1 and 10 μM significantly inhibited the H2O2–induced reduction in cell viability. Exposure of HUVECs to donepezil (1 μM) for 2 h upregulated HIF-1α expression. |
| Animal experiment [1,3]: | |
Animal models | Male Lister Hooded rats, adult male NMRI mice |
Dosage form | Intraperitoneal administration, 1 mg/kg |
Application | In Male Lister Hooded rats, donepezil dose-dependently increased salivation and tremor with an ED50 of 6 μmol/kg. In adult male NMRI mice, donepezil (1 mg/kg) improved recognition performances. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. Snape M F, Misra A, Murray T K, et al. A comparative study in rats of the in vitro and in vivo pharmacology of the acetylcholinesterase inhibitors tacrine, donepezil and NXX-066[J]. Neuropharmacology, 1999, 38(1): 181-193. [2]. Huang Z H, Guo W, Zhang L L, et al. Donepezil protects endothelial cells against hydrogen peroxide‐induced cell injury[J]. CNS neuroscience & therapeutics, 2012, 18(2): 185-187. [3].Freret T, Bouet V, Quiedeville A, et al. Synergistic effect of acetylcholinesterase inhibition (donepezil) and 5-HT 4 receptor activation (RS67333) on object recognition in mice[J]. Behavioural brain research, 2012, 230(1): 304-308. | |
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| Cas No. | 120011-70-3 | SDF | Download SDF |
| Chemical Name | 2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxy-2,3-dihydroinden-1-one;hydrochloride | ||
| Canonical SMILES | COC1=C(C=C2C(=C1)CC(C2=O)CC3CCN(CC3)CC4=CC=CC=C4)OC.Cl | ||
| Formula | C24H30ClNO3 | M.Wt | 415.95 |
| Solubility | ≥10.4mg/mL in H2O | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Donepezil Hydrochloride (Donepezil HCL) is a novel, potent and selective inhibitor of acetylcholinesterase (AChE), an enzyme possibly involved in cognitive dysfunction of patients suffering Alzheimer’s disease (AD), with the half maximal inhibition concentration IC50 value of 6.7 nM [1].
Donepezil HCL is a piperidine-class AChE inhibitor containing an N-benzylpiperdine and an indanone moiety, which confers it a longer and more selective action against AchE as compared to BuChE (IC50: 7.4 μM) [1].
Donepezil HCL has been approved by FDA for the treatment of AD, in which it has improved cognitive function of mild to severe moderate AD patients and exhibited excellent tolerability without hepatotoxicity [1].
Reference
References:[1] Sugimoto H, Ogura H, Arai Y, Limura Y, Yamanishi Y. Research and development of donepezil hydrochloride, a new type of acetylcholinesterase inhibitor. Jpn J Pharmacol. 2002 May;89(1):7-20.
