Name: Varenicline (CP 526555) dihydrochloride
Brand: Selleck Chemicals
SKU: S0717
Rating: 5 (1 reviews)

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

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

Varenicline (CP 526555) dihydrochloride Related Products

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Signaling Pathway

AChR Signaling Pathway

Choose Selective AChR Inhibitors

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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT04317300	Withdrawn	Vaping	Mayo Clinic	February 1 2023	Early Phase 1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

References

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	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

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
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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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Tech Support

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Handling Instructions

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