Varenicline (Tartrate)

Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation[1][2][3][4][5].

Product Specifications

CAS Number

[375815-87-5]

Product Name Alternative

CP 526555-18

UNSPSC

12352005

Hazard Statement

H302, H400

Target

ERK; nAChR; p38 MAPK

Type

Reference compound

Related Pathways

MAPK/ERK Pathway; Membrane Transporter/Ion Channel; Neuronal Signaling; Stem Cell/Wnt

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease; Others; Cancer

Assay Protocol

https://www.medchemexpress.com/Varenicline-Tartrate.html

Concentration

10mM

Purity

99.96

Solubility

DMSO : 14.29 mg/mL (ultrasonic) |H2O : 20 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(O)[C@H](O)[C@@H](O)C(O)=O.C1(C2CC3CNC2)=C3C=C(N=CC=N4)C4=C1

Molecular Formula

C17H19N3O6

Molecular Weight

361.35

Precautions

H302, H400

References & Citations

[1] Koegelenberg CF, et al. Efficacy of varenicline combined with nicotine replacement therapy vs varenicline alone for smoking cessation: a randomized clinical trial. JAMA. 2014 Jul;312 (2) :155-61. |[2]Magnus CJ, et al. Ultrapotent chemogenetics for research and potential clinical applications. Science. 2019;364 (6436) :eaav5282.|[3]Koga M, et al. Varenicline promotes endothelial cell migration by lowering vascular endothelial-cadherin levels via the activated α7 nicotinic acetylcholine receptor-mitogen activated protein kinase axis. Toxicology. 2017;390:1-9.|[4] Ren J, et al. Countering Opioid-induced Respiratory Depression in Male Rats with Nicotinic Acetylcholine Receptor Partial Agonists Varenicline and ABT 594. Anesthesiology. 2020 May;132 (5) :1197-1211.|[5]Mello NK, et al. Effects of chronic varenicline treatment on nicotine, cocaine, and concurrent nicotine+cocaine self-administration. Neuropsychopharmacology. 2014 Apr;39 (5) :1222-31.|[6]Rollema H, et al. Varenicline has antidepressant-like activity in the forced swim test and augments sertraline's effect. Eur J Pharmacol. 2009 Mar 1;605 (1-3) :114-6.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

Launched

Available Sizes

Curated Selection

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