| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| 250mg | |||
| 500mg | |||
| Other Sizes |
| Targets |
Varenicline targets the α4β2 neuronal nicotinic acetylcholine receptor (nAChR) subtype, where it acts as a partial agonist. It also acts as a full agonist at the α7 nAChR. It has a Ki of 0.12±0.02 for nAChR binding.
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| ln Vitro |
In cell-free systems, Varenicline's activity is assessed by its ability to bind to the nAChR. This is measured using radioligand binding assays. Its agonistic activity is measured by its ability to activate the receptor in functional assays. In vitro, Varenicline blocks the direct agonist effects of nicotine on nAChRs while simultaneously stimulating these receptors in a more moderate and controlled manner. It enhances neuronal differentiation of neural progenitor cells.
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| ln Vivo |
Treatment with varenicline (0.5-2 mg/kg/day; subcutaneous injection; twice daily; for 14 days; male Wistar rats) demonstrated significantly greater availability of DRD2/3 in the ventral striatum, ca. 11%, but rats treated with varenicline alone at doses of 1 mg/kg/day and 2 mg/kg/day showed substantial increases in DRD2/3 availability in the dorsal striatum by 12.5% and 13.2%, respectively. Varenicline can elicit a dose-dependent and sustained rise in DRD2/3 in the rat striatum, notably in the ventral striatum [1].
In vivo, Varenicline is effective in reducing nicotine craving and withdrawal symptoms. It is used as a smoking cessation aid. It has also been investigated for its utility in alcohol use disorder. It restores memory deficits in a mouse dementia model. |
| Enzyme Assay |
In vitro receptor binding assays are performed using membrane preparations from cells expressing the nAChR. The compound's ability to displace a radiolabeled ligand is measured to determine its binding affinity (Ki).
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| Cell Assay |
Cells expressing nAChRs are treated with Varenicline. Its agonistic activity is measured by assessing receptor activation, such as by measuring ion flux or changes in membrane potential. Its effects on neuronal differentiation are evaluated by measuring neurite outgrowth.
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| Animal Protocol |
Animal/Disease Models: 80 male Wistar rats (250-300 g) [1]
Doses: 0.5 mg/kg/day, 1 mg/kg/day, or 2 mg/kg/day twice (two times) daily; for 14 days Experimental Results: Abdominal DRD2/3 availability in the lateral striatum was Dramatically increased by approximately 11%, while rats treated with doses of only 1 and 2 mg/kg/day demonstrated a significant increase in DRD2/3 availability in the dorsal striatum of 12.5% , respectively 13.2%. In vivo efficacy is evaluated in animal models of nicotine dependence. Varenicline is administered, and its effects on nicotine self-administration and withdrawal symptoms are measured. Its effects on memory are assessed in dementia models. |
| ADME/Pharmacokinetics |
Varenicline is orally bioavailable. It is metabolized in the liver, and its pharmacokinetic properties are well-characterized. Its half-life allows for twice-daily dosing. It is excreted primarily in urine.
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| Toxicity/Toxicokinetics |
Common side effects of Varenicline include nausea, headache, and insomnia. It is generally well-tolerated. It has a boxed warning for neuropsychiatric symptoms. Its safety profile is well-established from clinical use.
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| References |
[1]. Crunelle CL, et al. Dose-dependent and sustained effects of varenicline on dopamine D2/3 receptor availability in rats. Eur Neuropsychopharmacol. 2011 Feb;21(2):205-10.
[2]. Kikkawa H, et al. Single- and multiple-dose pharmacokinetics of the selective nicotinic receptor partial agonist, varenicline, in healthy Japanese adult smokers. J Clin Pharmacol. 2011 Apr;51(4):527-37. [3]. Pachas GN, Cather C, Pratt SA et al. Varenicline for Smoking Cessation in Schizophrenia: Safety and Effectiveness in a 12-Week, Open-Label Trial. J Dual Diagn. 2012;8(2):117-125. [4]. Bordia T, Hrachova M, Chin M et al. 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. |
| Additional Infomation |
See also: Vareniclan hydrochloride (note moved to).
Varenicline is a widely used prescription drug for smoking cessation. It was initially approved by the FDA in 2006. It is considered a first-line treatment and is also being studied for other indications. |
| Molecular Formula |
C₁₃H₁₄CLN₃
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|---|---|
| Molecular Weight |
247.72
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| Exact Mass |
247.087
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| Elemental Analysis |
C, 54.94; H, 5.32; Cl, 24.95; N, 14.79
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| CAS # |
230615-23-3
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| Related CAS # |
Varenicline;249296-44-4
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| PubChem CID |
50878597
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| Appearance |
Light yellow to khaki solid powder
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| LogP |
2.934
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
17
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| Complexity |
254
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1(C2CC3CNC2)=C3C=C(N=CC=N4)C4=C1.Cl
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| InChi Key |
ZUCZFANFKYSVKF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H13N3.ClH/c1-2-16-13-5-11-9-3-8(6-14-7-9)10(11)4-12(13)15-1;/h1-2,4-5,8-9,14H,3,6-7H2;1H
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| Chemical Name |
5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca-2,4,6,8,10-pentaene;hydrochloride
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| Synonyms |
CP-526555 hydrochlorideCP 526555 hydrochlorideCP 526555-18 CP-526555 18 CP 526555 18 CP52655518 Varenicline tartrate Chantix Champix
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
H2O : ~50 mg/mL (~201.84 mM)
DMSO : ≥ 2.5 mg/mL (~10.09 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (403.68 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0368 mL | 20.1841 mL | 40.3682 mL | |
| 5 mM | 0.8074 mL | 4.0368 mL | 8.0736 mL | |
| 10 mM | 0.4037 mL | 2.0184 mL | 4.0368 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.
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.
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