Varenicline tartrate

Name: Varenicline tartrate
Brand: Tocris Bioscience
SKU: 3754

Tocris Bioscience, part of Bio-Techne | Catalog # 3754

Citations (36)

COA / SDS

Selective α4β2 nAChR partial agonist; orally active

Key Product Details

Description:	Selective α4β2 nAChR partial agonist; orally active
Chemical Name:	7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine tartrate
Purity:	≥99% (HPLC)
Molecular Weight:	361.37

View Full Technical Details for Varenicline tartrate

Technical Data
Citations

Biological Activity for Varenicline tartrate

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.

Compound Libraries for Varenicline tartrate

Varenicline tartrate is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.

Technical Data for Varenicline tartrate

M. Wt	361.37
Formula	C₁₃H₁₃N₃.C₄H₆O₆
Storage	Desiccate at RT
Purity	≥99% (HPLC)
CAS Number	375815-87-5
PubChem ID	5310966
InChi Key	JQSHBVHOMNKWFT-DTORHVGOSA-N
Smiles	OC(C(O)C(O)=O)C(O)=O.C1(C=C([C@H]4CNC[C@@H]3C4)C3=C2)=C2N=CC=N1

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

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for Varenicline tartrate

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	water	36.14	100
	DMSO	18.07	50

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 will affect the solvent volumes required to prepare stock solutions.

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

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References for Varenicline tartrate

References are publications that support the biological activity of the 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