Home Neuronal Signaling AChR antagonist Varenicline For research use only.

Varenicline

Synonyms: Chantix, Champix,CP 526555

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). Varenicline also acts as an agonist of 5-HT3 serotonine receptors.

Varenicline Chemical Structure

Varenicline Chemical Structure

CAS: 249296-44-4

Purity & Quality Control

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

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Biological Activity

Description 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). Varenicline also acts as an agonist of 5-HT3 serotonine receptors.
Targets
α4β2 receptors [1] 5-HT3 receptor [2]
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NCT04317300 Withdrawn Vaping Mayo Clinic February 1 2023 Early Phase 1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 211.26 Formula

C13H13N3
CAS No. 249296-44-4 SDF --
Smiles C1NCC2CC1C3=CC4=NC=CN=C4C=C23
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 42 mg/mL ( (198.8 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 42 mg/mL

Water : 3 mg/mL


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In vivo
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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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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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