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Varenicline Tartrate (CP 526555-18)

Alias: CP 526555-18; CP52655518; Varenicline tartrate;CP-526555 18; CP 526555 18;Chantix; Champix
Cat No.:V1203 Purity: ≥98%
Varenicline Tartrate (CP-526555 18; CP 526555 18;Chantix; Champix), the tartrate salt of varenicline, is a potent partial agonist of nicotinic AChR (acetylcholine receptor) used for smoke-cessation and nicotine addiction.
Varenicline Tartrate (CP 526555-18)
Varenicline Tartrate (CP 526555-18) Chemical Structure CAS No.: 375815-87-5
Product category: AChR Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
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Other Forms of Varenicline Tartrate (CP 526555-18):

  • Varenicline
Official Supplier of:
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Top Publications Citing lnvivochem Products
Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Varenicline Tartrate (CP-526555 18; CP 526555 18; Chantix; Champix), the tartrate salt of varenicline, is a potent partial agonist of nicotinic AChR (acetylcholine receptor) used for smoke-cessation and nicotine addiction.

Biological Activity I Assay Protocols (From Reference)
ln Vitro

In vitro activity: Varenicline is a partial agonist with 45% of nicotines maximal efficacy atalpha4beta2 nAChRs in HEK cells expressing nAChRs. Varenicline is a potent, partial agonist at alpha4beta2 receptors, with an EC50 of 2.3 mM and an efficacy (relative to acetylcholine) of 13.4%. Varenicline has lower potency and higher efficacy at alpha3beta4 receptors, with an EC50 of 55 mM and an efficacy of 75%.

ln Vivo
Varenicline has significantly lower (40-60%) efficacy than nicotine in stimulating [(3)H]-dopamine release from rat brain slices in vitro and in increasing dopamine release from rat nucleus accumbens in vivo, while it is more potent than Nicotine. Varenicline effectively attenuates the nicotine-induced dopamine release to the level of the effect of Varenicline alone, consistent with partial agonism. Varenicline reduces nicotine self-administration in rats and supports lower self-administration break points than nicotine. Varenicline dose-dependently reduces nicotine self-administration and attenuates both nicotine prime and combined nicotine prime plus nicotine-paired cue-induced reinstatement. Varenicline, a partial agonist at thealpha4beta2 nAChRs, reduces nicotine intake and was recently approved as a smoking cessation aid. Varenicline selectively reduces ethanol but not sucrose seeking using an operant self-administration drinking paradigm and also decreases voluntary ethanol but not water consumption in animals chronically exposed to ethanol for 2 months before Varenicline treatment.
Animal Protocol

Rats
References
Neuropharmacology.2007 Mar;52(3):985-94;Psychopharmacology (Berl).2010 Feb;208(3):365-76.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C13H13N3.C4H6O6
Molecular Weight
361.35
CAS #
375815-87-5
Related CAS #
Varenicline;249296-44-4
Appearance
Typically exists as solids (or liquids in special cases) at room temperature
SMILES
O([H])[C@@]([H])(C(=O)O[H])[C@]([H])(C(=O)O[H])O[H].N1([H])C([H])([H])C2([H])C3=C([H])C4C(C([H])=C3C([H])(C1([H])[H])C2([H])[H])=NC([H])=C([H])N=4
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
Chemical Name
(6R,10S)-7,8,9,10-tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline (2R,3R)-2,3-dihydroxysuccinate
Synonyms
CP 526555-18; CP52655518; Varenicline tartrate;CP-526555 18; CP 526555 18;Chantix; Champix
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO:<1 mg/mL
Water:72 mg/mL (199.3 mM)
Ethanol:<1 mg/mL
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 1.43 mg/mL (3.96 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.3 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 1.43 mg/mL (3.96 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: 10 mg/mL (27.67 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C).


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.7674 mL 13.8370 mL 27.6740 mL
5 mM 0.5535 mL 2.7674 mL 5.5348 mL
10 mM 0.2767 mL 1.3837 mL 2.7674 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • Varenicline Tartrate

    The effects of varenicline on food self-administration under a fixed ratio schedule of reinforcement.Psychopharmacology (Berl).2010 Feb;208(3):365-76.


    Varenicline Tartrate

    The effects of varenicline on nicotine self-administration under a fixed ratio schedule of reinforcement.
  • Varenicline Tartrate

    The effects of varenicline on reinstatement of nicotine-seeking.Psychopharmacology (Berl).2010 Feb;208(3):365-76.
  • Varenicline Tartrate

    Dose–response functions for nicotine and varenicline prime-induced reinstatement of nicotine seeking.Psychopharmacology (Berl).2010 Feb;208(3):365-76.
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