Home Neuronal Signaling AChR agonist Varenicline (CP 526555) dihydrochloride For research use only.

Varenicline (CP 526555) dihydrochloride

Synonyms: Chantix, Champix,CP 526555 dihydrochloride

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 Chemical Structure

Varenicline (CP 526555) dihydrochloride Chemical Structure

CAS No. 866823-63-4

Purity & Quality Control

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

Varenicline (CP 526555) dihydrochloride Related Products

Signaling Pathway

AChR Signaling Pathways

AChR Signaling Pathway

Biological Activity

Description 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.
Targets
α4β2 nAChR [1]
(Cell-free assay)		 α7 nAChRs [1]
(Cell-free assay)		 α3β4 nAChR [1]
(Cell-free assay)
2.3 μM(EC50) 18 μM(EC50) 55 μM(EC50)
In Vivo
In vivo

Varenicline induces dose-dependent and sustains increases in striatal DRD2/3 in rats, particularly in the ventral striatum.[2]
Animal Research Animal Models male Wistar rat
Dosages 0.5, 1 or 2mg/kg/day
Administration s.c.
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NCT04317300 Withdrawn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

Chemical Information & Solubility

Molecular Weight 284.18 Formula

C13H15Cl2N3
CAS No. 866823-63-4 SDF --
Smiles C1C2CNCC1C3=CC4=NC=CN=C4C=C23.Cl.Cl
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 57 mg/mL ( (200.57 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 57 mg/mL

Ethanol : 29 mg/mL


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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