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Rivastigmine AChR inhibitor

Cat.No.S4687

Rivastigmine (SDZ-ENA 713, Exelon) is a cholinesterase inhibitor with IC50 of 5.5 μM. It inhibits acetylcholinesterase (IC50 = 4.15 µM) and butyrylcholinesterase (IC50 = 37 nM).
Rivastigmine AChR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 250.34

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Chemical Information, Storage & Stability

Molecular Weight 250.34 Formula

C14H22N2O2

 Storage (From the date of receipt) 2 years  -20°C  liquid
CAS No. 123441-03-2 Download SDF Storage of Stock Solutions

Synonyms SDZ-ENA 713, Exelon Smiles CCN(C)C(=O)OC1=CC=CC(=C1)C(C)N(C)C

Solubility

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
cholinesterase [1]
In vivo
Preclinical biochemical studies indicates that rivastigmine has central nervous system selectivity over peripheral inhibition. It ameliorates memory impairment in rats with forebrain lesions. The drug is rapidly absorbed orally, with a bioavailability of 0.355 and low protein binding (40%). Its elimination halflife is less than 2 hours, and it is converted to an inactive metabolite at the site of action, bypassing hepatic metabolic pathways. Its disposition essentially is unaltered in patients with renal or hepatic impairment. It also has dosedependent effects on AChE inhibition[1].
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05768126 Recruiting
Depressive Disorder
UMC Utrecht|ZonMw: The Netherlands Organisation for Health Research and Development|St. Antonius Hospital|Tergooi Hospital
 September 29 2021 Phase 4
NCT01585272 Completed
Alzheimer''s Dementia
Novartis Pharmaceuticals|Novartis
 August 2012 Phase 4
NCT01073319 Completed
Methamphetamine Dependence|Substance Abuse|Methamphetamine Abuse
Baylor College of Medicine|National Institute on Drug Abuse (NIDA)
 July 2009 Phase 1
NCT01312363 Completed
Alzheimer''s Disease
Seoul National University Hospital|Seoul National University Bundang Hospital|Seoul St. Mary''s Hospital|Korea University|Bobath Memorial Hospital|Chung-Ang University Hosptial Chung-Ang University College of Medicine|Hanyang University|Kwandong University Myongji Hospital|Inha University Hospital|SungAe General Hospital|Ewha Womans University|Inje University|Hanyang University Seoul Hospital|Kyunghee University Medical Center|Hallym University Medical Center|Pusan National University Hospital|Konyang University Hospital|Wonkwang University Sanbon Medical Center|Yong-in Hyoja Geriatric Hospital|Jeju National University|Dong-A University Hospital
 June 2009 --
NCT00624663 Completed
Rivastigmine Toxicity
Tel-Aviv Sourasky Medical Center|Medical Corps Israel Defense Force
 January 2009 Not Applicable

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