Home Neuronal Signaling AChR agonist Varenicline (CP 526555) dihydrochloride

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Varenicline (CP 526555) dihydrochloride AChR agonist

Cat.No.S0717

Varenicline (CP 526555, Chantix, Champix,CP 526555 dihydrochloride) dihydrochloride is a potent, partial agonist of α4β2 nicotinic acetylcholine receptor (nAChR) and α3β4 nAChR with EC50 of 2.3 μM and 55 μM, respectively. Varenicline dihydrochloride is a potent, full agonist of α7 nAChRs with EC50 of 18 μM. Varenicline is a prescription medication used for smoking cessation.
Varenicline (CP 526555) dihydrochloride AChR agonist Chemical Structure

Chemical Structure

Molecular Weight: 284.18

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Quality Control

Batch: S071701 DMSO]57 mg/mL]false]Water]57 mg/mL]false]Ethanol]29 mg/mL]false Purity: 99.08%
99.08

Solubility

In vitro
Batch:

DMSO : 57 mg/mL (200.57 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 57 mg/mL

Ethanol : 29 mg/mL

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In vivo
Batch:

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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.

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Chemical Information, Storage & Stability

Molecular Weight 284.18 Formula

C13H15Cl2N3

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 866823-63-4 -- Storage of Stock Solutions

Synonyms Chantix, Champix,CP 526555 dihydrochloride SMILES C1C2CNCC1C3=CC4=NC=CN=C4C=C23.Cl.Cl

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Mechanism of Action

Targets/IC50/Ki
α4β2 nAChR
(Cell-free assay)
2.3 μM(EC50)
α7 nAChRs
(Cell-free assay)
18 μM(EC50)
α3β4 nAChR
(Cell-free assay)
55 μM(EC50)
In vivo

Varenicline induces dose-dependent and sustains increases in striatal DRD2/3 in rats, particularly in the ventral striatum.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-08-25)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07783555 NOT_YET_RECRUITING
Cannabis Abuse
Medical University of South Carolina
 2026-12-01 PHASE2
NCT07040566 RECRUITING
E-cigarette Use; Vaping; Nicotine Dependence
Yale University
 2025-10-14 PHASE2
NCT06966362 RECRUITING
Veterans; Tobacco Use Disorder; Cigarette Smoking; Tobacco Dependence
VA Office of Research and Development
 2026-08-17 PHASE4
NCT07714200 NOT_YET_RECRUITING
Tobacco Use Disorder
VA Office of Research and Development
 2027-03-01
NCT07099638 RECRUITING
Smoking Cessation
University of Oklahoma
 2026-07-21 PHASE2
NCT06609369 RECRUITING
Tobacco Use; Tobacco Cessation; Insomnia
Yale University
 2025-04-21 PHASE2

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