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Donepezil HCl(Aricept) is a selective and effective AChE inhibitor for bAChE and hAChE (IC50: 8.12/11.6 nM).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $44 | In Stock | |
50 mg | $63 | In Stock | |
100 mg | $85 | In Stock | |
200 mg | $129 | In Stock | |
500 mg | $216 | In Stock | |
1 mL x 10 mM (in DMSO) | $68 | In Stock |
Description | Donepezil HCl(Aricept) is a selective and effective AChE inhibitor for bAChE and hAChE (IC50: 8.12/11.6 nM). |
Targets&IC50 | AChE (bovine):8.12 nM, AChE (human):11.6 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. |
Alias | E2020, Donepezil HCl, BNAG, Aricept |
Molecular Weight | 415.96 |
Formula | C24H29NO3·HCl |
Cas No. | 120011-70-3 |
Smiles | Cl.COc1c(OC)cc2C(=O)C(CC3CCN(Cc4ccccc4)CC3)Cc2c1 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 4.2 mg/mL (10.1 mM), Sonication is recommended. ![]() H2O: 31.2 mg/mL (75.01 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
In Vivo Formulation | Saline: 5.82 mg/mL (13.99 mM), In vivo: Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.![]() | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO/H2O
H2O
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