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MedKoo Cat#: 318974 | Name: Varenicline tartrate
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Varenicline is a nicotinic receptor partial agonist—it stimulates nicotine receptors more weakly than nicotine itself does. In this respect it is similar to cytisine and different from the nicotinic antagonist, bupropion, and nicotine replacement therapies (NRTs) like nicotine patches and nicotine gum. Varenicline displays full agonism on α7 nicotinic acetylcholine receptors and is a partial agonist on the α4β2, α3β4, and α6β2 subtypes. In addition, it is a weak agonist on the α3β2 containing receptors. Varenicline's partial agonism on the α4β2 receptors rather than nicotine's full agonism produces less effect of dopamine release than nicotine's. This α4β2 competitive binding reduces the ability of nicotine to bind and stimulate the mesolimbic dopamine system—similar to the method of action of buprenorphine in the treatment of opioid addiction.

Chemical Structure

Varenicline tartrate
Varenicline tartrate
CAS#375815-87-5 (tartrate)

Theoretical Analysis

MedKoo Cat#: 318974

Name: Varenicline tartrate

CAS#: 375815-87-5 (tartrate)

Chemical Formula: C17H19N3O6

Exact Mass: 0.0000

Molecular Weight: 361.35

Elemental Analysis: C, 56.51; H, 5.30; N, 11.63; O, 26.57

Price and Availability

Size Price Availability Quantity
10mg USD 400.00
25mg USD 600.00
50mg USD 950.00
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Related CAS #
375815-87-5 (tartrate) 866823-63-4 (HCl) 249296-44-4 (free base)
Synonym
Varenicline tartrate; Chantix; Champix; HSDB7591; HSDB-7591; HSDB 7591; CP 526555; CP-526555; CP526555;
IUPAC/Chemical Name
(6R,10S)-7,8,9,10-tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline (2R,3R)-2,3-dihydroxysuccinate
InChi Key
TWYFGYXQSYOKLK-CYUSMAIQSA-N
InChi Code
InChI=1S/C13H13N3.C4H6O6/c1-2-16-13-5-11-9-3-8(6-14-7-9)10(11)4-12(13)15-1;5-1(3(7)8)2(6)4(9)10/h1-2,4-5,8-9,14H,3,6-7H2;1-2,5-6H,(H,7,8)(H,9,10)/t8-,9+;1-,2-/m.1/s1
SMILES Code
C1[C@@H]2CNC[C@H]1C3=CC4=NC=CN=C4C=C23.[C@@H]([C@H](C(=O)O)O)(C(=O)O)O
Appearance
White to beige crystalline powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Related CAS# CAS#375815-87-5 ( Varenicline tartrate) CAS#249296-44-4 (Varenicline free base) CAS#230615-23-3 ( Varenicline HCl)

Preparing Stock Solutions

The following data is based on the product molecular weight 361.35 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.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Wen CC, Baker N, Paul R, Hill E, Hunt K, Li H, Gray K, Neelon B. A Bayesian beta-binomial piecewise growth mixture model for longitudinal overdispersed binomial data. Stat Methods Med Res. 2024 Oct;33(10):1859-1876. doi: 10.1177/09622802241279109. Epub 2024 Oct 7. PMID: 39370804. 2: Aryanpur M, Ghorbani R, Rashno S, Heydari G, Kazempour-Dizaji M, Hessami Z, Ghorbani N. The Effect of Varenicline on Smoking Cessation in Hospitalized Patients: A Systematic Review and Meta-Analysis. Addict Health. 2024 May;16(2):122-129. doi: 10.34172/ahj.2024.1328. Epub 2024 May 1. PMID: 39051033; PMCID: PMC11264481. 3: Wen CC, Baker N, Paul R, Hill E, Hunt K, Li H, Gray K, Neelon B. A Bayesian zero-inflated beta-binomial model for longitudinal data with group-specific changepoints. Stat Med. 2024 Jan 15;43(1):125-140. doi: 10.1002/sim.9945. Epub 2023 Nov 9. PMID: 37942694. 4: Lang AE, Patel U, Fitzpatrick J, Lee T, McFarland M, Good CB. Association of the Chantix Recall With US Prescribing of Varenicline and Other Medications for Nicotine Dependence. JAMA Netw Open. 2023 Feb 1;6(2):e2254655. doi: 10.1001/jamanetworkopen.2022.54655. PMID: 36745457. 5: King A, Vena A, de Wit H, Grant JE, Cao D. Effect of Combination Treatment With Varenicline and Nicotine Patch on Smoking Cessation Among Smokers Who Drink Heavily: A Randomized Clinical Trial. JAMA Netw Open. 2022 Mar 1;5(3):e220951. doi: 10.1001/jamanetworkopen.2022.0951. PMID: 35244704; PMCID: PMC8897753. 6: Carson-Chahhoud KV, Smith BJ, Peters MJ, Brinn MP, Ameer F, Singh K, Fitridge R, Litt J, Edwards D, Koblar SA, Jannes J, Veale AJ, Goldsworthy S, Hnin K, Esterman AJ. Correction: Two-year efficacy of varenicline tartrate and counselling for inpatient smoking cessation (STOP study): A randomized controlled clinical trial. PLoS One. 2021 Dec 30;16(12):e0262188. doi: 10.1371/journal.pone.0262188. Erratum for: PLoS One. 2020 Apr 29;15(4):e0231095. doi: 10.1371/journal.pone.0231095. PMID: 34969062; PMCID: PMC8717977. 7: Kim E, Hwang JG, Park SJ, Han JY, Choi YS, Park SR, Yu KS, Park MK, Lee S. Pharmacokinetic comparison between tablet of varenicline tartrate and orally disintegrating film of varenicline salicylate in healthy subjects. Int J Clin Pharmacol Ther. 2021 Jun;59(6):478-484. doi: 10.5414/CP203953. PMID: 33704052. 8: Xie L, Xiao L, Kuang D, Jiang Y, Yang Y. [Influencing factors on smoking cessation among outpatients from the National Central Subsidy Smoking Cessation Clinic Project, in 2015-2018]. Zhonghua Liu Xing Bing Xue Za Zhi. 2020 Jun 10;41(6):890-895. Chinese. doi: 10.3760/cma.j.cn112338-20191104-00780. PMID: 32564555. 9: Miranda R Jr, O'Malley SS, Treloar Padovano H, Wu R, Falk DE, Ryan ML, Fertig JB, Chun TH, Muvvala SB, Litten RZ. Effects of Alcohol Cue Reactivity on Subsequent Treatment Outcomes Among Treatment-Seeking Individuals with Alcohol Use Disorder: A Multisite Randomized, Double-Blind, Placebo-Controlled Clinical Trial of Varenicline. Alcohol Clin Exp Res. 2020 Jul;44(7):1431-1443. doi: 10.1111/acer.14352. Epub 2020 May 25. PMID: 32363592; PMCID: PMC7572549. 10: Carson-Chahhoud KV, Smith BJ, Peters MJ, Brinn MP, Ameer F, Singh K, Fitridge R, Koblar SA, Jannes J, Veale AJ, Goldsworthy S, Hnin K, Esterman AJ. Two-year efficacy of varenicline tartrate and counselling for inpatient smoking cessation (STOP study): A randomized controlled clinical trial. PLoS One. 2020 Apr 29;15(4):e0231095. doi: 10.1371/journal.pone.0231095. Erratum in: PLoS One. 2021 Dec 30;16(12):e0262188. doi: 10.1371/journal.pone.0262188. PMID: 32348306; PMCID: PMC7190140. 11: Park JW, Kim KA, Son H, Jung J, Park JY. Pharmacokinetic comparisons of two different varenicline formulations in humans: Varenicline tartrate versus varenicline oxalate
. Int J Clin Pharmacol Ther. 2020 Feb;58(2):121-127. doi: 10.5414/CP203574. PMID: 31699211. 12: Gray KM, Baker NL, McClure EA, Tomko RL, Squeglia LM, Saladin ME, Carpenter MJ. Efficacy and Safety of Varenicline for Adolescent Smoking Cessation: A Randomized Clinical Trial. JAMA Pediatr. 2019 Dec 1;173(12):1146-1153. doi: 10.1001/jamapediatrics.2019.3553. PMID: 31609433; PMCID: PMC6802269. 13: Gökçe B, Sarıoğlu N, Gençer N, Arslan O. Association of human serum paraoxonase-1 with some respiratory drugs. J Biochem Mol Toxicol. 2019 Dec;33(12):e22407. doi: 10.1002/jbt.22407. Epub 2019 Oct 3. PMID: 31581362. 14: Hernández Zenteno RJ, Lara DF, Venegas AR, Sansores RH, Pineda JR, Trujillo FF, Pérez Padilla JR, Matera MG, Cazzola M. Varenicline for long term smoking cessation in patients with COPD. Pulm Pharmacol Ther. 2018 Dec;53:116-120. doi: 10.1016/j.pupt.2018.11.001. Epub 2018 Nov 3. PMID: 30399395. 15: Lu Y, Sun X, Song F, Wang L, Song M, Hang T. Impurity profiling of varenicline tartrate by LC-QTOF mass spectrometric techniques during drug development. J Pharm Biomed Anal. 2018 Jun 5;155:306-313. doi: 10.1016/j.jpba.2018.03.055. Epub 2018 Apr 3. PMID: 29679875. 16: Drovandi AD, Robertson SG, Malau-Aduli BS, Teague PA, Glass BD. Addressing varenicline adherence through repackaging in a dose administration aid. Integr Pharm Res Pract. 2017 Jun 23;6:131-135. doi: 10.2147/IPRP.S132091. PMID: 29354559; PMCID: PMC5774312. 17: O'Malley SS, Zweben A, Fucito LM, Wu R, Piepmeier ME, Ockert DM, Bold KW, Petrakis I, Muvvala S, Jatlow P, Gueorguieva R. Effect of Varenicline Combined With Medical Management on Alcohol Use Disorder With Comorbid Cigarette Smoking: A Randomized Clinical Trial. JAMA Psychiatry. 2018 Feb 1;75(2):129-138. doi: 10.1001/jamapsychiatry.2017.3544. PMID: 29261824; PMCID: PMC5838706. 18: Cui Y, Engelmann JM, Xian J, Minnix JA, Lam CY, Karam-Hage M, Cinciripini PM, Robinson JD. Pharmacological intervention and abstinence in smokers undergoing cessation treatment: A psychophysiological study. Int J Psychophysiol. 2018 Jan;123:25-34. doi: 10.1016/j.ijpsycho.2017.12.001. Epub 2017 Dec 6. PMID: 29223599; PMCID: PMC5759327. 19: Tan R, Bölükbaşi Hatip F, Açikalin Ö, Yamauchi A, Kataoka Y, Hatip-Al-Khatib I. Effect of varenicline on behavioral deficits in a rat model of Parkinson's disease induced by unilateral 6-hydroxydopamine lesion of substantia nigra. Behav Pharmacol. 2018 Jun;29(4):327-335. doi: 10.1097/FBP.0000000000000355. PMID: 29064842. 20: Zhou C, Wu L, Liu Q, An H, Jiang B, Zuo F, Zhang L, He Y. Evaluation of smoking cessation intervention in patients with chronic diseases in smoking cessation clinics. Medicine (Baltimore). 2017 Oct;96(42):e7459. doi: 10.1097/MD.0000000000007459. PMID: 29049178; PMCID: PMC5662344.