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Rivastigmine AChR inhibitor

Name: Rivastigmine
Brand: Selleck Chemicals
SKU: S4687
Availability: InStock
Rating: 5 (2 reviews)

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).

Chemical Structure

Molecular Weight: 250.34

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Quality Control

Batch: S468701 Purity: 99.98%

Cited in Nature Medicine for its top-tier quality
COA
SDS
Datasheet

99.98

Related Targets	Adrenergic Receptor 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Other AChR Inhibitors	PNU-120596 Benzethonium Chloride Arecoline HBr Otilonium Bromide Lycorine Hyoscyamine (-)-Huperzine A (HupA) Nitenpyram Cytisine Chelidonine

Solubility

In vitro
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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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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	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	SDZ-ENA 713, Exelon			Smiles	CCN(C)C(=O)OC1=CC=CC(=C1)C(C)N(C)C

Mechanism of Action

Targets/IC₅₀/Ki	cholinesterase
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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/10641971/ [2] https://pubmed.ncbi.nlm.nih.gov/21440537/ [3] https://pubmed.ncbi.nlm.nih.gov/11914613/

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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