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Chemical Structure| 120014-06-4 Chemical Structure| 120014-06-4

Structure of Donepezil
CAS No.: 120014-06-4

Chemical Structure| 120014-06-4

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Donepezil is a centrally acting reversible AchE inhibitor with IC50 of 8.12 nM and 11.6 nM for bAChE and hAChE, respectively, a medication used to treat Alzheimer's disease.

Synonyms: E2020 free base; Aricept; HSDB 7743

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Product Citations

Product Citations

Petzer, Anél ; Petzer, Jacobus P ; Cloete, Stephanus J ;

Abstract: (AChE) is present in the venom of Elapid snakes, except the Mambas. Although the physiological role of in snake venom is uncertain, it may contribute to acute neuromuscular paralysis following envenomation. With the aim of repurposing clinically used drugs for snakebite envenoming, this study investigated the inhibition of from snake species of Southern Africa. Hemachatus haemachatus and Naja nivea venom presented with high activity, which was inhibited by , galantamine and with IC50 values ranging from 0.49 to 3.73 μM.

Keywords: ; ; Galantamine ; ; Venom ; Snakebite

Purchased from AmBeed: ; 357-70-0

Alternative Products

Product Details of Donepezil

CAS No. :120014-06-4
Formula : C24H29NO3
M.W : 379.49
SMILES Code : C1=C2C(=CC(=C1OC)OC)CC(C2=O)CC4CCN(CC3=CC=CC=C3)CC4
Synonyms :
E2020 free base; Aricept; HSDB 7743
MDL No. :MFCD00912833
InChI Key :ADEBPBSSDYVVLD-UHFFFAOYSA-N
Pubchem ID :3152

Safety of Donepezil

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • AChE

    hAChE, IC50:11.6 nM

    bAChE, IC50:8.12 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
OPC-DRG neuron co-culture 10 μM 9 days Donepezil promotes myelination in OPC-DRG neuron co-culture. Acta Pharmacol Sin. 2019 Nov;40(11):1386-1393.
Primary OPCs 2.5–20 μM 4 days Donepezil significantly increases the percentage of MBP+ OLs generated from primary OPCs. Acta Pharmacol Sin. 2019 Nov;40(11):1386-1393.
Mouse 6-3 microglial cells 5 μM 12 hours Pretreatment with donepezil suppressed the TNFα-induced sustained intracellular Ca2+ elevation J Neuroinflammation. 2017 Dec 22;14(1):258.
Mouse primary microglial cells 5 μM 12 hours Pretreatment with donepezil suppressed the TNFα-induced sustained intracellular Ca2+ elevation J Neuroinflammation. 2017 Dec 22;14(1):258.
Rat HAPI microglial cells 5 μM 12 hours Pretreatment with donepezil suppressed the TNFα-induced sustained intracellular Ca2+ elevation J Neuroinflammation. 2017 Dec 22;14(1):258.
APPsw-SY5Y cells 10 μmol/L 2 hours To evaluate the inhibitory effect of donepezil on copper-induced Aβ1-42 production, results showed that donepezil significantly reduced Aβ1-42 production Acta Pharmacol Sin. 2016 Nov;37(11):1401-1412.
Th17 cells 5 μM 48 hours To evaluate the effect of Donepezil on Th17 cell differentiation. Results showed that Donepezil significantly reduced the expression of IL17A in Th17 cells and inhibited the activation of the JAK2-STAT3 signaling pathway. Theranostics. 2023 Mar 21;13(6):1826-1842.
NPC-derived OPCs 20 μM 4.5 days Donepezil significantly promotes OPC to OL differentiation, increasing the percentage of MBP+ cells. Acta Pharmacol Sin. 2019 Nov;40(11):1386-1393.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rat Passive avoidance test model Oral 0.1 mg/kg Single dose Evaluate the effect of Donepezil in the passive avoidance test model Cell. 2021 Nov 24;184(24):5886-5901.e22
C57BL/6 mice BLM-induced lung fibrosis mouse model Intraperitoneal injection 1 mg/kg Once daily for 21 days To evaluate the effect of Donepezil on BLM-induced lung fibrosis and pulmonary hypertension. Results showed that Donepezil significantly improved pulmonary artery and RV remodeling, reduced lung fibrosis, and inhibited Th17 cell infiltration and activation. Theranostics. 2023 Mar 21;13(6):1826-1842.
Male mice VGLUT3T8I/T8I mutant mice Intraperitoneal injection 0.3 mg/kg Daily throughout the entire ABA paradigm To evaluate the effect of donepezil on reversing the self-starvation phenotype in VGLUT3T8I/T8I mice, showing that donepezil effectively reversed the self-starvation behavior in mutant mice. Nat Commun. 2024 Jul 7;15(1):5691
Mice VAChTcKO mice Intraperitoneal injection 0.3 mg/kg Chronic treatment Increasing cholinergic signaling by AChE inhibition was fully effective to treat the anorexia-like phenotype in VAChTcKO mice. J Clin Invest. 2020 Dec 1;130(12):6616-6630
Mice Scopolamine-induced memory-deficient mouse model Intracalvariosseous administration 5 mg/kg Single administration, lasting four weeks To evaluate the long-term cognitive improvement effect of DPZ@LAM, results showed that a single ICO of DPZ@LAM significantly recovered cognitive function in scopolamine-induced memory-deficient mice, along with decreased acetylcholinesterase activity and increased brain-derived neurotrophic factor. Theranostics. 2024 Oct 14;14(17):6708-6725
Mouse Drd1a-tdTomato/Drd2-mVenus double transgenic mice Subcutaneous injection 0.4 mg/kg Single dose To investigate the enhancement of aversive learning by donepezil through M1R-PKC-PAK signaling Mol Psychiatry. 2022 Aug;27(8):3479-3492.
Mice Chronic stress model Intraperitoneal injection 1.0 mg/kg Single administration Investigated the effects of Donepezil on cognitive and emotional deficits in chronically stressed mice. Results showed Donepezil alone improved cognitive deficits but exacerbated anxiety-like behaviors, while combined with vHPC M1 receptor blockade rescued both phenotypes. Sci Adv. 2024 Nov 8;10(45):eado1508
C57BL/6 mice Cuprizone-induced demyelination model Intraperitoneal injection 1.5 and 5 mg/kg Daily for 1–3 weeks Donepezil significantly promotes remyelination in vivo, reducing demyelination area and increasing myelin formation. Acta Pharmacol Sin. 2019 Nov;40(11):1386-1393.
Mice 3xTg and 5xFAD mouse models Intraperitoneal injection 1.0 and 2.0 mg/kg Daily for 4 weeks Low-dose donepezil significantly ameliorated MS-hTau-induced spatial memory deficits and reduced tau accumulation, with more prominent effects than high dose. Clin Transl Med. 2021 Jun;11(6):e428
C57BL6/J mice AlCl3-induced Alzheimer's disease model Nasal administration 30 mg/kg Once daily for 7 weeks To evaluate the improvement of cognitive function and memory ability in AlCl3-induced AD mice by GH/CeO2NPs, results showed significant improvement. Int J Mol Sci. 2024 Apr 11;25(8):4262

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01633593 Elderly|Delirium of Unknown (A... More >>xis III) Etiology|Intensive Care (ICU) Myopathy Less << PHASE4 TERMINATED 2025-07-16 FAMEMA, Marilia, Sao Paulo, 17... More >>50000, Brazil Less <<
NCT00196690 Stroke|Aphasia PHASE4 COMPLETED 2025-03-05 Gabinete Berthier y Martínez, ... More >>Malaga, Spain. Centro de Investigaciones Médico-Sanitarias (CIMES), UNiversity of Malaga, Malaga, Spain., Malaga, 29001, Spain Less <<
NCT02206620 Parkinson's Disease PHASE2 COMPLETED 2025-07-17 Oregon Health & Science Univer... More >>sity, Portland, Oregon, 97239-3098, United States Less <<
NCT02158910 Alzheimer's Disease COMPLETED 2025-06-16 Busan, Korea, Republic of|Chun... More >>gcheongbuk-do, Korea, Republic of|Chungcheongnam-do, Korea, Republic of|Daegu, Korea, Republic of|Gangwon-do, Korea, Republic of|Gwangju, Korea, Republic of|Gyeonggji-do, Korea, Republic of|Gyeongsangbuk-do, Korea, Republic of|Gyeongsangnam-do, Korea, Republic of|Jeju-do, Korea, Republic of|Jeollabuk-do, Korea, Republic of|Jeollanam-do, Korea, Republic of|Seoul, Korea, Republic of Less <<
NCT00533065 Elderly COMPLETED 2025-07-09 Ludwig Boltzmann Institute, Vi... More >>enna, 1220, Austria Less <<
NCT00530478 Stroke UNKNOWN - Samsung Medical Center, Seoul,... More >> 135-710, Korea, Republic of Less <<
NCT01276080 Healthy PHASE1 COMPLETED 2025-12-09 Novum Pharmaceutical Research ... More >>Services, Las Vegas, Nevada, 89121, United States Less <<
NCT00142324 Alzheimer's Disease PHASE4 UNKNOWN 2025-12-05 Queen Elizabeth Psychiatric Ho... More >>spital, Birmingham, B15 2QZ, United Kingdom|Department of Psychiatry for the Elderly, Leicester General Hospital, Leicester, LE5 4PW, United Kingdom|Institute of Psychiatry, King's College, London, London, SE5 8AF, United Kingdom|Old Age Psychiatry, Wythenshawe Hospital, Manchester, Manchester, M23 9LT, United Kingdom|Institute for Ageing and Health, Newcastle General Hospital, Newcastle, Newcastle upon Tyne, NE4 6BE, United Kingdom|Department of Psychiatry, Warneford Hospital, Oxford, Oxford, OX3 7JX, United Kingdom|MARC, Moorgreen Hospital, Southamptom, Southampton, S030 3JB, United Kingdom|Department of Old Age Psychiatry, Victoria Hospital, Swindon, Swindon, SN1 4HZ, United Kingdom Less <<
NCT00566501 Alzheimer's Disease PHASE3 COMPLETED 2010-04-01 Apex Research Institute, Santa... More >> Ana, California, 92705, United States Less <<
NCT00381381 Alzheimer's Disease PHASE4 COMPLETED 2008-12-31 Seoul National University Bund... More >>ang Hospital, Bundang, Korea, Republic of|Hallym University Medical Center, Changwon, Korea, Republic of|Kangwon National University Hospital, Chuncheon, Korea, Republic of|Kunkuk University Chungju Hospital, Chungju, Korea, Republic of|Kyungpook National University Hospital, Daegu, Korea, Republic of|Chungnam National University Hospital, Daejeon, Korea, Republic of|Gyeonggi Province Geriatric Hospital, Gyeonggi, Korea, Republic of|Uijeongbu St. Mary's Hospital, Gyeonggi, Korea, Republic of|Jeju National University Hospital, Jeju, Korea, Republic of|Jeonju City Welfare Hospital, Jeonju, Korea, Republic of|Gyeongsang National University Hospital, Jinju, Korea, Republic of|Inje University Pusan Paik Hospital, Pusan, Korea, Republic of|Kunkuk University Hospital, Seoul, Korea, Republic of|Seoul National University Hospital, Seoul, Korea, Republic of|Seoul St. Mary's Hospital, Seoul, Korea, Republic of Less <<
NCT06518941 Anorexia Nervosa PHASE2 NOT_YET_RECRUITING 2025-06-26 New York State Psychiatric Ins... More >>titute, New York, New York, 10032, United States Less <<
NCT00220896 Cognitively Normal Elderly Ind... More >>ividuals Less << PHASE4 COMPLETED 2025-03-09 Deps. of Psychiatry and Anaest... More >>hesiology, Tech. Universitaet Munich, Munich, D-81675, Germany Less <<
NCT00465283 Schizophrenia|Schizoaffective ... More >>Disorder|Schizophreniform Disorder Less << PHASE4 UNKNOWN 2025-01-10 Beer Yaakov MHC, Beer Yaacov, ... More >>70350, Israel Less <<
NCT02450786 Parkinson's Disease PHASE2 UNKNOWN 2025-08-19 Severance Hospital, Seoul, 120... More >>-752, Korea, Republic of Less <<
NCT01923558 Healthy PHASE1 COMPLETED 2025-11-10 Algorithme Pharma Inc., Mount ... More >>Royal, Quebec, H3P 3P1, Canada Less <<
NCT00230568 Alzheimer's Disease PHASE4 COMPLETED 2025-12-07 21st Century Neurology, Phoeni... More >>x, Arizona, 85013, United States|Alzheimer's Disease and Cognitive Disorders Clinic at Barrow Neurology Institute, Phoenix, Arizona, 85013, United States|Pacific Sleep Medicine Services, Inc., El Centro, California, 92243, United States|Pacific Sleep Medicine Services, Inc., Los Angeles, California, 90048, United States|Pacific Sleep Medicine Services, Inc., San Diego, California, 92121, United States|Parkinson's Disease Movement Disorders Center - Boca Raton, Boca Raton, Florida, 33486, United States|Bradenton Research Center, Bradenton, Florida, 34205, United States|MD Clinical, Hallandale Beach, Florida, 33009, United States|Eastern Research, Hialeah, Florida, 33013, United States|Berma Research Group, Hialeah, Florida, 33016, United States|Cuervo Research Group, Miami, Florida, 33143, United States|Seth Hochman, MD, Miami, Florida, 33156, United States|Collier Neurologic Specialists, Naples, Florida, 34102, United States|Segal Institute for Clinical Research, North Miami, Florida, 33161, United States|Ocala Neurodiagnostic Center, Ocala, Florida, 34471, United States|Memory Disorder Center, Pompano Beach, Florida, 33064, United States|Liliana Montoya, MD, Port Charlotte, Florida, 33952, United States|Roskamp Institute Memory Clinic, Tampa, Florida, 33617, United States|Palm Beach Neurology, West Palm Beach, Florida, 33407, United States|Cleveland Clinic Florida, Weston, Florida, 33331, United States|The Northwestern Alzheimer's Center, Chicago, Illinois, 60611, United States|Rush Alzheimer's Disease Center, Chicago, Illinois, 60612, United States|Lozano, Cosme, MD, Joliet, Illinois, 60435, United States|University of Nevada School of Medicine,, Las Vegas, Nevada, 89102, United States|ClinSearch Inc., Kenilworth, New Jersey, 07033, United States|University of New Mexico School of Medicine, Department of Psychiatry, Albuquerque, New Mexico, 87131, United States|New York University School of Medicine, Aging and Dementia Research Center, New York, New York, 10016, United States|The Burke Rehabilitation Hospital, White Plains, New York, 10605, United States|North Carolina Neuropsychiatry, PA, Charlotte, North Carolina, 28209, United States|Clinical Research Associates, Inc., Oklahoma City, Oklahoma, 73118, United States|Clinical Research Center, Jenkintown, Pennsylvania, 19046, United States|The Penn Ralston Center, University of Pennsylvania, Philadelphia, Pennsylvania, 19104, United States|University of Texas Mental Sciences Insitute, Houston, Texas, 77030, United States|Christopher Ticknor, MD, San Antonio, Texas, 78229, United States|University of Texas, Health Science Center-San Antonio, San Antonio, Texas, 78229, United States Less <<
NCT01014858 Parkinson's Disease PHASE3 TERMINATED 2025-09-14 Newcastle, Newcastle Upon Tyne... More >>, Tyne and Wear, NE4 5PL, United Kingdom|Royal United Hospital (RUH) Bath NHS, Bath, BA1 3NG, United Kingdom|Sandwell and West Birmingham NHS Foundation Trust, Birmingham, B18 7QH, United Kingdom|Steps and Pines, Southmead Hospital, Bristol, BS10 5NB, United Kingdom|Pennine Acute Hospitals NHS Trust, Bury, BL9 7TD, United Kingdom|Cambridge Centre for Brain Repair, Cambridge, CB2 0PY, United Kingdom|Dr Lakmali Sugathapala, Derby, DE22 3NE, United Kingdom|Royal Bournemouth & Christchurch Hospitals NHS Foundation Trust, Dorset, BH23 2JX, United Kingdom|NHS Greater Glasgow and Clyde, Glasgow, G51 4TF, United Kingdom|Dr Pippa Metcalf, Gloucester, Gloucester, United Kingdom|Llandudno Hospital, Betsi Cadwaladr University Health Board & School of Medical Sciences, Llandudno, LL30 1LB, United Kingdom|King's College Hospital NHS Foundtion Trust, London, SE59RS, United Kingdom|Manchester Mental Health & Social Care NHS Trust, Manchester, M8 5RB, United Kingdom|Milton Keynes, Milton Keynes, MK6 5LD, United Kingdom|Royal Gwent Hospital, Newport, NP20 2UB, United Kingdom|North Tyneside General Hospital, Northumberland, NE29 8NH, United Kingdom|Norfolk and Norwich University Hospitals NHS Foundation Trust, Norwich, NR4 7UY, United Kingdom|Oxford University Hospitals NHS Foundation Trust, Oxford, OX3 9DU, United Kingdom|Plymouth Hospitals NHS Trust, Plymouth, PL6 8DH, United Kingdom|Poole Hospital NHS Trust, Poole, BH15 2JB, United Kingdom|Southampton General Hospital, Southampton, SO16 6YD, United Kingdom|Dr Dhakam, Surrey, KT16 0PZ, United Kingdom Less <<
NCT00452868 Brain and Central Nervous Syst... More >>em Tumors|Cognitive/Functional Effects|Long-term Effects Secondary to Cancer Therapy in Children|Neurotoxicity|Psychosocial Effects of Cancer and Its Treatment|Radiation Toxicity Less << EARLY_PHASE1 COMPLETED 2025-02-10 Tufts-NEMC Cancer Center, Bost... More >>on, Massachusetts, 02111, United States|Wake Forest University Comprehensive Cancer Center, Winston-Salem, North Carolina, 27157-1096, United States Less <<
NCT02415062 Parkinson's Disease PHASE2 UNKNOWN 2025-12-17 Inje university, busan paik ho... More >>spital, Busan, Korea, Republic of Less <<
NCT00805792 Ischemic Stroke PHASE2 COMPLETED 2025-09-10 Mayo Clinic, Jacksonville, Flo... More >>rida, 32224, United States Less <<
NCT00934531 Falls|Gait|Balance|Mild Cognit... More >>ive Impairment (MCI) Less << COMPLETED 2025-01-19 St. Joseph's Health Care Londo... More >>n, Parkwood Hospital, London, Ontario, N6C 5J1, Canada Less <<
NCT00103948 Cognitive Impairment PHASE2 COMPLETED 2025-02-07 Jose Biller, M.D., Maywood, Il... More >>linois, 60152, United States|New York University School of Medicine, New York, New York, 10016, United States|Woodville, South Australia, 5011, Australia|Malaga, 29010, Spain Less <<
NCT01923259 Healthy PHASE1 COMPLETED 2025-12-10 Algorithme Pharma Inc., Mount ... More >>Royal, Quebec, H3P 3P1, Canada Less <<
NCT01951118 Alzheimer Disease|Mild Cogniti... More >>ve Impairment|Delirium, Dementia, Amnestic, Cognitive Disorders Less << PHASE4 COMPLETED 2025-05-19 New York State Psychiatric Ins... More >>titute, New York, New York, 10032, United States Less <<
NCT04661280 Alzheimer Disease, Early Onset PHASE3 RECRUITING 2025-08-26 Cognitive Neurology Center, Pa... More >>ris, 75010, France Less <<
NCT01276067 Healthy PHASE1 COMPLETED 2025-12-09 Novum Pharmaceutical Research ... More >>Services, Pittsburgh,, Pennsylvania, United States Less <<
NCT00182884 Postoperative Complications|De... More >>lirium Less << PHASE4 COMPLETED 2025-04-07 Methodist Hospital, Clarian He... More >>alth Partners, Indianapolis, Indiana, 46202, United States Less <<
NCT02787746 Alzheimer's Disease PHASE4 COMPLETED 2025-03-19 Beijing Friendship Hospital, C... More >>apital Medical University, Beijing, Beijing, China Less <<
NCT00174382 Dementia, Vascular|Dementia, M... More >>ixed Less << PHASE3 TERMINATED 2025-04-08 Pfizer Investigational Site, B... More >>elvedere, Alberta, T5C 0A3, Canada|Pfizer Investigational Site, Edmonton, Alberta, T5A 4L8, Canada|Pfizer Investigational Site, Edmonton, Alberta, T6A 0A5, Canada|Pfizer Investigational Site, Abbotsford, British Columbia, V2S 3P8, Canada|Pfizer Investigational Site, Coquitlam, British Columbia, V3K 3P4, Canada|Pfizer Investigational Site, Victoria, British Columbia, V8T 5G1, Canada|Pfizer Investigational Site, Winnipeg, Manitoba, R2H 0R8, Canada|Pfizer Investigational Site, Saint John, New Brunswick, E2L 3L6, Canada|Pfizer Investigational Site, Amherst, Nova Scotia, B4H 4R7, Canada|Pfizer Investigational Site, Halifax, Nova Scotia, B3H 2E1, Canada|Pfizer Investigational Site, Pictou, Nova Scotia, B0K 1H0, Canada|Pfizer Investigational Site, Burlington, Ontario, L7M 4Y1, Canada|Pfizer Investigational Site, Corunna, Ontario, N0N 1G0, Canada|Pfizer Investigational Site, Fort Erie, Ontario, L2A 1Z3, Canada|Pfizer Investigational Site, Hawkesbury, Ontario, K6A 1A1, Canada|Pfizer Investigational Site, North Bay, Ontario, P1B 2H3, Canada|Pfizer Investigational Site, Ottawa, Ontario, K1N 5C8, Canada|Pfizer Investigational Site, Ottawa, Ontario, K2C 3R2, Canada|Pfizer Investigational Site, Ottawa, Ontario, K2G 3Y5, Canada|Pfizer Investigational Site, Peterborough, Ontario, K9H 2P4, Canada|Pfizer Investigational Site, Sarnia, Ontario, N7T 4X3, Canada|Pfizer Investigational Site, Toronto, Ontario, M3B 2W7, Canada|Pfizer Investigational Site, Beauport, Quebec, G1J 2G3, Canada|Pfizer Investigational Site, Cowansville, Quebec, J2K 2X9, Canada|Pfizer Investigational Site, L'Ancienne-Lorette, Quebec, G2E 2X1, Canada|Pfizer Investigational Site, Montréal, Quebec, H1T 2M4, Canada|Pfizer Investigational Site, Rimouski, Quebec, G5L 9A8, Canada|Pfizer Investigational Site, St-Jean-sur-Richelieu, Quebec, J2W 2A3, Canada|Pfizer Investigational Site, St. Leonard, Quebec, H1S 3A9, Canada|Pfizer Investigational Site, Regina, Saskatchewan, S4P 3X1, Canada Less <<
NCT02222727 Aneurysmal Subarachnoid Hemorr... More >>hage|Delayed Neurological Deficit|Delayed Cerebral Ischemia|Vasospasm Less << PHASE2 TERMINATED 2025-11-16 St George's University of Lond... More >>on, London, SW17 0RE, United Kingdom Less <<
NCT00182845 Postoperative Complications|De... More >>lirium Less << PHASE4 COMPLETED 2025-04-07 University Hospital, Clarian H... More >>ealth Partners, Indianapolis, Indiana, 46202, United States Less <<
NCT00030979 Parkinson Disease PHASE4 COMPLETED 2025-03-05 National Institute of Neurolog... More >>ical Disorders and Stroke (NINDS), Bethesda, Maryland, 20892, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.64mL

0.53mL

0.26mL

13.18mL

2.64mL

1.32mL

26.35mL

5.27mL

2.64mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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