Donepezil HCl

Catalog No.S2462 Batch:S246201

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Technical Data

Formula

C24H29NO3.HCl
Molecular Weight 416 CAS No. 120011-70-3
Solubility (25°C)* In vitro Water 31 mg/mL (74.51 mM)
Ethanol 2 mg/mL (4.8 mM)
DMSO 1 mg/mL (2.4 mM)
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Donepezil HCl is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM , respectively.This product is not soluble in PBS solution. Please do not dissolve it in PBS for administration.
Targets
bAChE [1] hAChE [1]
8.12 nM 11.6 nM
In vitro

Donepezil HCl 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. A recent study shows that Donepezil can protect human umbilical vein endothelial cells (HUVECs) against H2O2-induced cell injury. This may be useful as a potential therapy for oxidative stress in cardiovascular and cerebrovascular diseases.

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. . 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 (0.1mg/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.

Protocol (from reference)

Animal Study:

[2]
  • Animal Models

    Male Lister Hooded rats

  • Dosages

    18 μM/kg

  • Administration

    Administered via i.p. or p.o.

References

  • https://pubmed.ncbi.nlm.nih.gov/11256231/
  • https://pubmed.ncbi.nlm.nih.gov/10193909/
  • https://pubmed.ncbi.nlm.nih.gov/22313947/
  • https://pubmed.ncbi.nlm.nih.gov/22348892/

Customer Product Validation

Donepezil-mediated eACh activity in vitro. After being cultured in serum-free EBM-2, HUVECs were treated with donepezil at a concentration of 10 umol/L for 24 hours. E and F: Representative images (x 400 magnification) of anti-ChAT and -VAChT immunofluorescence. Scale bar: 50 um. ChAT indicates choline acetyltransferase; eACh, endothelium-derived acetylcholine; EBM-2, endothelial basal medium 2; HUVECs, human umbilical vein endothelial cells; PCR, polymerase chain reaction; VAChT, vesicular acetylcholine transporter.

Data from [ J Am Heart Assoc , 2014 , 3(3), e000804 ]

Inhibition studies of known inhibitors against BACE1. a Dose-response curves for compounds inhibition of BACE1 in the MMSA (microfluidics-based mobility shift assay).

Data from [ , , Anal Bioanal Chem, 2017, 409(28):6635-6642 ]

Selleck's Donepezil HCl Has Been Cited by 23 Publications

Aging-related Repositioned Drugs, Donepezil and Sildenafil Citrate, Increase Apoptosis of Anti-mitotic Drug-resistant KBV20C Cells Through Different Molecular Mechanisms [ Anticancer Research, September 2018, 5149-5157] PubMed: 30194162
Aging-related Repositioned Drugs, Donepezil and Sildenafil Citrate, Increase Apoptosis of Anti-mitotic Drug-resistant KBV20C Cells Through Different Molecular Mechanisms [ Anticancer Research, September 15, 2018, 5149-5157] PubMed: 30194162
Arterial Baroreflex Dysfunction Impairs Ischemia-Induced Angiogenesis [ Journal of the American Heart Association, May 12, 2014, e000804] PubMed: 24820655
Intratarget Microdosing for Deep Phenotyping of Multiple Drug Effects in the Live Brain [ Frontiers in Bioengineering and Biotechnology, March 18, 2022, 855755] PubMed: 35372313
Antidementia medication acetylcholinesterase inhibitors have therapeutic benefits on osteoporotic bone by attenuating osteoclastogenesis and bone resorption [ Journal of Cellular Physiology, August 2023, 1823-1835] PubMed: 37334837
Cholinergic signaling to CA1 astrocytes controls fear extinction [ Science Advances, April 4, 2025, eads7191] PubMed: 40184457
Cholinergic signaling to CA1 astrocytes controls fear extinction [ Sci Adv, 2025, 11(14):eads7191] PubMed: 40184457
Inhibition of Th17 cells by donepezil ameliorates experimental lung fibrosis and pulmonary hypertension [ Theranostics, 2023, 13(6):1826-1842] PubMed: 37064881
Inhibition of Th17 cells by donepezil ameliorates experimental lung fibrosis and pulmonary hypertension [ Theranostics, 2023, 1826-1842] PubMed: 37064881
Antidementia medication acetylcholinesterase inhibitors have therapeutic benefits on osteoporotic bone by attenuating osteoclastogenesis and bone resorption [ J Cell Physiol, 2023, 10.1002/jcp.31057] PubMed: 37334837

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.