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: 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

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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NCT04317300 Withdrawn Vaping Mayo Clinic February 1 2023 Early Phase 1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 Active not recruiting Cannabis Use Disorder Medical University of South Carolina January 31 2020 Phase 2

Chemical lnformation & 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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