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Varenicline α4β2 nAChRs antagonist

Catalog No.B1140
Size Price Stock Qty
5mg
$70.00
In stock
25mg
$210.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

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Chemical structure

Varenicline

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Chemical Properties

Cas No. 249296-44-4 SDF Download SDF
Chemical Name (6R)-7,8,9,10-tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline
Canonical SMILES [H]C1(C([H])([H])N([H])C2([H])[H])C([H])([H])[[email protected]]2([H])C3=C([H])C4=NC([H])=C([H])N=C4C([H])=C13
Formula C13H13N3 M.Wt 211.26
Solubility Soluble in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

Varenicline is a partial agonist/antagonist of α4β2 nicotinic acetylcholine receptor [1].

Varenicline is a manufactured tartrate salt, it is a partial agonist of α4β2 nAChRs. The affinity(0.15 nM) of varenicline with α4β2 nAChRs is much more higher than with other nAChR subtypes. Through the binding, varenicline prevents nicotine from occupying the receptors and subsequently inhibit nicotine-induced dopaminergic activation. So varenicline is used for smoking cessation. In healthy adult smokers, varenicline does not undergo significant hepatic metabolism and the clearance(>90%) is predominantly renal. It is shown that the amphetamine administration may have decrease the efficacy of varenicline [1].

References:
[1] Garrison GD, Dugan SE. Varenicline: a first-line treatment option for smoking cessation. Clin Ther. 2009 Mar;31(3):463-91.