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Rivastigmine AChR inhibitor

Name: Rivastigmine
Brand: Selleck Chemicals
SKU: S4687
Availability: InStock
Rating: 5 (3 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).

Rivastigmine AChR inhibitor Chemical Structure

Quality Control

Batch: S468701 Purity: 99.98%

Cited in Nature Medicine for its top-tier quality
COA
SDS/MSDS
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 Palmatine Lycorine Nitenpyram PNU 282987 HCl Chelidonine Hyoscyamine

Solubility

In vitro
Batch:

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5mg/ml (19.97mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.71mg/ml (2.84mM)	Taking the 1 mL working solution as an example, add 50 μL of 14.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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 (From the date of receipt)	2 years -20°C liquid
Synonyms	SDZ-ENA 713, Exelon			SMILES	CCN(C)C(=O)OC1=CC=CC(=C1)C(C)N(C)C

Read more about storage stability stock solution CAS number SMILES

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 2025-06-05)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04366518	RECRUITING	Hallucinations, Auditory; Psychosis	Yale University	2021-07-15	EARLY_PHASE1
NCT06382649	RECRUITING	Anticholinergic Toxicity	Washington University School of Medicine	2026-06	PHASE2
NCT06399679	SUSPENDED	Anticholinergic Toxicity	Washington University School of Medicine	2024-11-04	PHASE2
NCT03454646	NOT_YET_RECRUITING	Alzheimer Disease; Cholinesterase Inhibitors	University Hospital, Bordeaux	2024-06-01	PHASE4
NCT07545382	COMPLETED	Anticholinergic Delirium; Clozapine Poisoning; Antipsychotic Toxicity; CNS Depression; Hypoactive Delirium; Tricyclic Antidepressant Poisoning; Procyclidine Induced Delirium	Alexandria University	2025-12-08	PHASE4
NCT07208344	RECRUITING	Alzheimer Disease (AD)	Anhui Provincial Hospital	2025-07-31	EARLY_PHASE1

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