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PZ0004 Sigma-Aldrich

Varenicline tartrate

≥98% (HPLC)

Synonym: 7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine tartrate, Champix

  • CAS Number 375815-87-5

  • Empirical Formula (Hill Notation) C13H13N3 · C4H6O6

  • Molecular Weight 361.35

  •  MDL number MFCD08460603

  •  PubChem Substance ID 329823673

  •  NACRES NA.77

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Properties

Related Categories Agonists, Approved Therapeutics/Drug Candidates, Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology,
Quality Level   100
assay   ≥98% (HPLC)
form   powder
mfr. no.   Pfizer®
color   white to beige
solubility   DMSO: >5 mg/mL
originator   Pfizer
storage temp.   room temp
SMILES string   O[C@H]([C@@H](O)C(O)=O)C(O)=O.C1NC[C@H]2C[C@@H]1c3cc4nccnc4cc23
InChI   1S/C13H13N3.C4H6O6/c1-2-16-13-5-11-9-3-8(6-14-7-9)10(11)4-12(13)15-1;5-1(3(7)8)2(6)4(9)10/h1-2,4-5,8-9,14H,3,6-7H2;1-2,5-6H,(H,7,8)(H,9,10)/t8-,9+;1-,2-/m.1/s1
InChI key   TWYFGYXQSYOKLK-CYUSMAIQSA-N

Description

Application

Varenicline tartrate has been used to investigate its effect on sensorimotor gating in rats under prepulse inhibition (PPI). It is suitable for use as a reference standard in capillary isotachophoresis (ITP) coupled on-line with capillary zone electrophoresis (CZE) for the quantification of varenicline metabolite in urine samples. It is also suitable for use for testing its effect on locomotor and nonlocomotor behavioral deficits in rats.

Packaging

5, 25 mg in glass bottle

Biochem/physiol Actions

Varenicline tartrate is a partial α4β2 nicotinic receptor agonist and α7 full agonist. Varenicline competitively binds to α4β2 receptors and partially stimulates without creating a full nicotine effect, while simultaneoudly blocking the ability of nicotine to bind to the receptors. Varenicline thus blocks the ability of nicotine to activate α4β2 receptors and stimulate the central nervous mesolimbic dopamine system, believed to be the neuronal mechanism underlying reinforcement and reward experienced upon smoking.

Features and Benefits

This compound is a featured product for ADME Tox research. Click here to discover more featured ADME Tox products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

This compound is also offered as part of Sigma′s Library of Pharmacologically Active Compounds (LOPAC®1280), a biologically annotated collection of high-quality, ready-to-screen compounds. Click here to learn more.

This compound is also offered as part of Sigma′s Library of Pharmacologically Active Compounds (LOPAC®Pfizer), a collection of 90 Pfizer-developed drugs and research tools. Click here to learn more.

This compound is featured on the Acetylcholine Receptors (Nicotinic) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Other Notes

This compound was developed by Pfizer for Neuroscience research. To learn more about Sigma′s partnership with Pfizer and view other authentic, high-quality Pfizer compounds, visit sigma.com/bsm-pfizer.

To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Legal Information

Sold for research purposes under agreement from Pfizer Inc.

LOPAC is a registered trademark of Sigma-Aldrich Co. LLC

Pfizer is a registered trademark of Pfizer, Inc.

Safety & Documentation

Safety Information

Symbol 
GHS09  GHS09
Signal word 
Warning
Hazard statements 
Precautionary statements 
RIDADR 
UN 3077 9 / PGIII
WGK Germany 
WGK 3
Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable

Documents

Certificate of Analysis (COA)

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Protocols & Articles

Articles

Acetylcholine Receptors (Nicotinic)

Nicotinic acetylcholine receptors (nAChRs) constitute a family of ligand-gated channels, originally classified on the basis of their activation by the alkaloid nicotine, with acetylcholine (ACh) bein...
Keywords: Analgesics, Diseases, Dopamine agents, Gene expression, Genetic, Inflammation, Ligands, Microscopy, Neurotransmission, Neurotransmitters, Scanning electron microscopy, Schizophrenia, Tissue microarrays, Transduction

Discover Bioactive Small Molecules for ADME/Tox

A significant number of drugs that fail in clinical trials have been associated with safety issues, including unexpected drug-drug interactions (DDI) or lack of efficacy due to poor pharmacokinetics....
Keywords: Absorption, Bioactive small molecules, Clinical, Metabolism

Pfizer Compounds for Neuroscience

From our library of Articles, Sigma-Aldrich presents Pfizer Compounds for Neuroscience

Peer-Reviewed Papers
15

References

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