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Varenicline Hydrochlorideα4β2 nicotinic receptor agonist

Varenicline Hydrochloride

Catalog No. B1141
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.

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Chemical structure

Varenicline Hydrochloride

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Chemical Properties

Cas No. 230615-23-3 SDF Download SDF
Chemical Name (6R)-7,8,9,10-tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline hydrochloride
Canonical SMILES Cl[H].[H]C1(C([H])([H])N([H])C2([H])[H])C([H])([H])[C@]2([H])C3=C([H])C4=NC([H])=C([H])N=C4C([H])=C13
Formula C13H14ClN3 M.Wt 247.72
Solubility Soluble in DMSO Storage Store at -20°C
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.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

Varenicline Hydrochloride is a partial agonist of α4β2 nicotinic receptor for smoking cessation [1].

Varenicline Hydrochloride has been reported to potently inhibit nAChR binding with the Ki values of 0.12±0.02 nM and 0.14±0.01 nM for α6β2* nAChR and α4β2* nAChR, respectively in rat striatum, 0.13±0.01 nM and 0.19±0.11 nM forα6β2* nAChR and α4β2* nAChR, respectively in monkey striatum. In addition, varenicline Hydrochloride has shown to be more potent in stimulating both α6β2* and α4β2* nAChRs compared with nicotine with the EC50 values of 0.007 and 0.086μM, respectively in rat striatum [1].

References:
[1] Bordia T1, Hrachova M, Chin M, McIntosh JM, Quik M. Varenicline is a potent partial agonist at α6β2* nicotinic acetylcholine receptors in rat and monkey striatum. J Pharmacol Exp Ther. 2012 Aug;342(2):327-34. doi: 10.1124/jpet.112.194852. Epub 2012 May 1.