Varenicline tartrate

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MedKoo CAT#: 318974

CAS#: 375815-87-5

Description: Varenicline tartrate is a prescription medication used to treat nicotine addiction. 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. As a partial agonist it both reduces cravings for and decreases the pleasurable effects of cigarettes and other tobacco products. Through these mechanisms it can assist some patients to quit smoking.

Chemical Structure

Varenicline tartrate
CAS# 375815-87-5

Theoretical Analysis

MedKoo Cat#: 318974
Name: Varenicline tartrate
CAS#: 375815-87-5
Chemical Formula: C17H19N3O6
Exact Mass:
Molecular Weight: 361.354
Elemental Analysis: C, 56.51; H, 5.30; N, 11.63; O, 26.57

Price and Availability

Size Price Availability Quantity
10.0mg USD 250.0 2 Weeks
25.0mg USD 450.0 2 Weeks
50.0mg USD 850.0 2 Weeks
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Related CAS #: 375815-87-5 (tartrate)   249296-44-4 (free)   230615-23-3 (HCl)  

Synonym: CP-526555-18; CP 526555 18; CP52655518; Varenicline tartrate; Chantix; Champix

IUPAC/Chemical Name: (6R,10S)-7,8,9,10-tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline (2R,3R)-2,3-dihydroxysuccinate


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

Preparing Stock Solutions

The following data is based on the product molecular weight 361.354 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

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1: Xiao D, Chu S, Wang C. Smoking cessation in Asians: focus on varenicline. Patient Prefer Adherence. 2015 Apr 13;9:579-84. doi: 10.2147/PPA.S60785. eCollection 2015. Review. Erratum in: Patient Prefer Adherence. 2015;9:1075. PubMed PMID: 25926724; PubMed Central PMCID: PMC4403695.

2: Thomas KH, Martin RM, Knipe DW, Higgins JP, Gunnell D. Risk of neuropsychiatric adverse events associated with varenicline: systematic review and meta-analysis. BMJ. 2015 Mar 12;350:h1109. doi: 10.1136/bmj.h1109. Review. PubMed PMID: 25767129; PubMed Central PMCID: PMC4357491.

3: Schwartz J, Fadahunsi O, Hingorani R, Mainali NR, Oluwasanjo A, Aryal MR, Donato A. Use of Varenicline in Smokeless Tobacco Cessation: A Systematic Review and Meta-Analysis. Nicotine Tob Res. 2015 Feb 2. pii: ntv010. [Epub ahead of print] Review. PubMed PMID: 25646351.

4: Hughes JR. Varenicline as a Cause of Suicidal Outcomes. Nicotine Tob Res. 2015 Jan 8. pii: ntu275. [Epub ahead of print] Review. PubMed PMID: 25572451.

5: Erwin BL, Slaton RM. Varenicline in the treatment of alcohol use disorders. Ann Pharmacother. 2014 Nov;48(11):1445-55. doi: 10.1177/1060028014545806. Epub 2014 Aug 5. Review. PubMed PMID: 25095786.

6: Chelladurai Y, Singh S. Varenicline and cardiovascular adverse events: a perspective review. Ther Adv Drug Saf. 2014 Aug;5(4):167-72. doi: 10.1177/2042098614530421. Review. PubMed PMID: 25083271; PubMed Central PMCID: PMC4110858.

7: Leaviss J, Sullivan W, Ren S, Everson-Hock E, Stevenson M, Stevens JW, Strong M, Cantrell A. What is the clinical effectiveness and cost-effectiveness of cytisine compared with varenicline for smoking cessation? A systematic review and economic evaluation. Health Technol Assess. 2014 May;18(33):1-120. doi: 10.3310/hta18330. Review. PubMed PMID: 24831822.

8: Romigi A, Vitrani G. Improvement of restless legs syndrome by varenicline as antismoking treatment. J Clin Sleep Med. 2013 Oct 15;9(10):1089-90. doi: 10.5664/jcsm.3092. Review. PubMed PMID: 24127155; PubMed Central PMCID: PMC3778182.

9: Haber SL, Boomershine V, Raney E. Safety of varenicline in patients with cardiovascular disease. J Pharm Pract. 2014 Feb;27(1):65-70. doi: 10.1177/0897190013504961. Epub 2013 Sep 30. Review. PubMed PMID: 24080536.

10: Nocente R, Vitali M, Balducci G, Enea D, Kranzler HR, Ceccanti M. Varenicline and neuronal nicotinic acetylcholine receptors: a new approach to the treatment of co-occurring alcohol and nicotine addiction? Am J Addict. 2013 Sep-Oct;22(5):453-9. doi: 10.1111/j.1521-0391.2013.12037.x. Epub 2013 May 15. Review. PubMed PMID: 23952890.

11: Santus P, Bassi L, Airoldi A, Giovannelli F, Radovanovic D. Varenicline and evaluated outcomes in smoking cessation programmes. Monaldi Arch Chest Dis. 2013 Mar;79(1):20-6. Review. PubMed PMID: 23741942.

12: Kurioka N. [On oral medications, especially varenicline]. Nihon Rinsho. 2013 Mar;71(3):487-92. Review. Japanese. PubMed PMID: 23631241.

13: Ahmed AI, Ali AN, Kramers C, Härmark LV, Burger DM, Verhoeven WM. Neuropsychiatric adverse events of varenicline: a systematic review of published reports. J Clin Psychopharmacol. 2013 Feb;33(1):55-62. doi: 10.1097/JCP.0b013e31827c0117. Review. PubMed PMID: 23277249.

14: Cerimele JM, Durango A. Does varenicline worsen psychiatric symptoms in patients with schizophrenia or schizoaffective disorder? A review of published studies. J Clin Psychiatry. 2012 Aug;73(8):e1039-47. doi: 10.4088/JCP.11r07410. Review. PubMed PMID: 22967780.

15: Mills EJ, Wu P, Lockhart I, Thorlund K, Puhan M, Ebbert JO. Comparisons of high-dose and combination nicotine replacement therapy, varenicline, and bupropion for smoking cessation: a systematic review and multiple treatment meta-analysis. Ann Med. 2012 Sep;44(6):588-97. doi: 10.3109/07853890.2012.705016. Epub 2012 Aug 6. Review. Erratum in: Ann Med. 2012 Sep;44(6):597. PubMed PMID: 22860882.

16: Prochaska JJ, Hilton JF. Risk of cardiovascular serious adverse events associated with varenicline use for tobacco cessation: systematic review and meta-analysis. BMJ. 2012 May 4;344:e2856. doi: 10.1136/bmj.e2856. Review. PubMed PMID: 22563098; PubMed Central PMCID: PMC3344735.

17: Christalla P, Dewenter M, El-Armouche A. [Effectiveness and safety of varenicline for smoking cessation]. Dtsch Med Wochenschr. 2012 May;137(18):940-4. doi: 10.1055/s-0032-1304895. Epub 2012 Apr 10. Review. German. PubMed PMID: 22492478.

18: Kassem MG, Al Hossaini AM. Varenicline. Profiles Drug Subst Excip Relat Methodol. 2012;37:389-411. doi: 10.1016/B978-0-12-397220-0.00010-6. Epub 2012 Mar 19. Review. PubMed PMID: 22469324.

19: Mahmoudi M, Coleman CI, Sobieraj DM. Systematic review of the cost-effectiveness of varenicline vs. bupropion for smoking cessation. Int J Clin Pract. 2012 Feb;66(2):171-82. doi: 10.1111/j.1742-1241.2011.02877.x. Review. PubMed PMID: 22257042.

20: Leung LK, Patafio FM, Rosser WW. Gastrointestinal adverse effects of varenicline at maintenance dose: a meta-analysis. BMC Clin Pharmacol. 2011 Sep 28;11:15. doi: 10.1186/1472-6904-11-15. Review. PubMed PMID: 21955317; PubMed Central PMCID: PMC3192741.

Additional Information

Related CAS#
CAS#375815-87-5 ( Varenicline tartrate)
CAS#249296-44-4 (Varenicline free base)
CAS#230615-23-3 ( Varenicline HCl)