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Varenicline AChR antagonist

Name: Varenicline
Brand: Selleck Chemicals
SKU: S6985
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S6985

Varenicline(CP 526555) is highly selective and blocks more potently to α4β2 receptors than to other common nicotinic receptors (>500-fold α3β4, >3,500-fold α7, >20,000-fold α1βγδ), or to non-nicotinic receptors and transporters (>2,000-fold). This compound also acts as an agonist of 5-HT3 serotonine receptors.

Chemical Structure

Molecular Weight: 211.26

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Quality Control

Batch: S698501 DMSO]42 mg/mL]false]Ethanol]42 mg/mL]false]Water]3 mg/mL]false Purity: 99.99%

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

99.99

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
Batch:

DMSO : 42 mg/mL (198.8 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 42 mg/mL

Water : 3 mg/mL

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:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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

Dosing volume per animal: μL

Number of animals:

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

% DMSO

Calculation results:

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	211.26	Formula	C₁₃H₁₃N₃	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	249296-44-4	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Chantix, Champix,CP 526555			Smiles	C1NCC2CC1C3=CC4=NC=CN=C4C=C23

Mechanism of Action

Targets/IC₅₀/Ki	α4β2 receptors 5-HT3 receptor
References	[1] https://pubmed.ncbi.nlm.nih.gov/31096265/ [2] https://pubmed.ncbi.nlm.nih.gov/25648658/

Clinical Trial Information

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

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04317300	Withdrawn	Vaping	Mayo Clinic	February 1 2023	Early Phase 1
NCT05576415	Completed	Dry Eye Disease	Ji Xing Pharmaceuticals (Shanghai) Co. Ltd.\|Oyster Point Pharma Inc.	December 7 2022	Phase 1
NCT03980561	Completed	Cannabis Use Disorder	Medical University of South Carolina	January 31 2020	Phase 2

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