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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C24H29NO3.HCl |
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分子量 | 416 | CAS No. | 120011-70-3 | ||||
Solubility (25°C)* | 体外 | Water | 5 mg/mL (12.01 mM) | ||||
DMSO | Insoluble | ||||||
Ethanol | Insoluble | ||||||
体内 (毎回新しく調製した物を用意してください) |
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* <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. |
製品説明 | Donepezil is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM , respectively. |
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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 H2O2-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 (0.1mg/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. [4] |
キナーゼアッセイ | AChE inhibitory activity | |
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PDGF receptor is immunoprecipitated from BALB/c 3T3 cell extracts with rabbit antiserum (for the murine PDGF receptor) for 2 hours on ice. Protein A-Sepharose beads are used to collect the antigen-antibody complexes. The immunoprecipitates are washed twice with TNET (50 mM Tris, pH 7.5, 140 mM NaCl, 5 mM EDTA, 1% Triton X-100), once with TNE (50 mM Tris, pH 7.5, 140 mM EDTA), and once with kinase buffer (20 mM Tris, pH 7.5,10 mM MgCl2). After stimulation with PDGF (50 ng/ml) at 4 °C for 10 minutes, different concentrations of the drug are added to the reaction mixture. PDGF receptor kinase activity is determined by incubation with 10 μCi [7-32P]-ATP and l μM ATP for 10 minutes at 4 °C. Immune complexes are separated by SDS-PAGE on 7.5% gels. | ||
動物実験 | 動物モデル | Male Lister Hooded rats |
投薬量 | 18 μM/kg | |
投与方法 | Administered via i.p. or p.o. |
Data from [Data independently produced by J Am Heart Assoc, 2014, 3(3), e000804]
Data from [Data independently produced by , , Anal Bioanal Chem, 2017, 409(28):6635-6642]
Inhibition of Th17 cells by donepezil ameliorates experimental lung fibrosis and pulmonary hypertension [ Theranostics, 2023, 13(6):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 |
Protective effect of Huanglianjiedu Decoction on microcystin-LR induced nerve injury [ Comp Biochem Physiol C Toxicol Pharmacol, 2023, 272:109698] | PubMed: 37442312 |
Intratarget Microdosing for Deep Phenotyping of Multiple Drug Effects in the Live Brain [ Front Bioeng Biotechnol, 2022, 10:855755] | PubMed: 35372313 |
A study of protein-drug interaction based on solvent-induced protein aggregation by fluorescence correlation spectroscopy [ Analyst, 2022, 10.1039/d2an00031h] | PubMed: 35253833 |
Donepezil Ameliorates Pulmonary Arterial Hypertension by Inhibiting M2-Macrophage Activation [ Front Cardiovasc Med, 2021, 8:639541] | PubMed: 33791350 |
Reduced TRPC6 mRNA levels in the blood cells of patients with Alzheimer's disease and mild cognitive impairment [Lu R Mol Psychiatry, 2018, 23(3):767-776] | PubMed: 28696436 |
Aging-related Repositioned Drugs, Donepezil and Sildenafil Citrate, Increase Apoptosis of Anti-mitotic Drug-resistant KBV20C Cells Through Different Molecular Mechanisms [Kim JY Anticancer Res, 2018, 38(9):5149-5157] | PubMed: 30194162 |
A microfluidics-based mobility shift assay to identify new inhibitors of β-secretase for Alzheimer's disease [Liu R Anal Bioanal Chem, 2017, 409(28):6635-6642] | PubMed: 28889204 |
Arterial baroreflex dysfunction impairs ischemia-induced angiogenesis [Hao C, et al J Am Heart Assoc, 2014, 3(3):e000804] | PubMed: 24820655 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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