Varenicline tartrate

Key Product Details

Product Description

Varenicline tartrate is an orally active, subtype-selective partial agonist at α4β2 nicotinic receptors (K_i values are 0.06, 240, 322 and 3540 nM for α4β2, α3β4, α7, α1βγδ receptors respectively). Reduces nicotine-evoked dopamine release in vitro and decreases nicotine self-administration in vivo. Also potently activates PSAM⁴-5-HT₃ and PSAM⁴-GlyR chimeric ion channels (EC₅₀ values are 4 and 1.6 nM, respectively)

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Product Specifications for Varenicline tartrate

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for Varenicline tartrate

The following data is based on the product molecular weight 361.37.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.77 mL	13.84 mL	27.67 mL
5 mM	0.55 mL	2.77 mL	5.53 mL
10 mM	0.28 mL	1.38 mL	2.77 mL
50 mM	0.06 mL	0.28 mL	0.55 mL

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 26 publications citing the usage of this product.

• Rollema Pharmacological profile of the α₄β₂ nicotinic acetylcholine receptor partial agonist varenicline, an effective smoking cessation aid. Neuropharmacology 2007 PMID: 17157884
• Rollema Preclinical pharmacology of the α4β2 nAChR partial agonist vareni. related to effects on reward, mood and cognition. Biochem.Pharmacol. 2009 PMID: 19501054
• Coe Varenicline: an α4β2 nicotinic receptor partial agonist for smoking cessation. J.Med.Chem. 2005 PMID: 15887955

Product Documents for Varenicline tartrate