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Varenicline (also known as CP 526555), an approved medication used to treat nicotine addiction, is a potent and selective α4β2 nicotinic receptor (nAChR) partial agonist. Varenicline is a partial agonist with 45% of nicotine's 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%. 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.
| ln Vitro |
Varenicline (1 μM, 24 hours) suppresses the rate of cell proliferation in RAW 264.7 macrophages as well as LPS-induced cytokine secretion (IL-1β, IL-6, and TNF α) [1]. Human adrenal chromaffin cells derived from male and female organ donors exhibit action potentials (Aps) in the absence of ACh activation when exposed to 250 nM vannicline [3]. By inhibiting VE-cadherin protein expression, vannicline (100 μM, 4 hours) increases HUVEC migration [4].
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| ln Vivo |
Varenicline (0.01-1 mg/kg subcutaneously, 3 days) injected subcutaneously at a dose of 0.5 mg/kg 10 minutes before to the onset of nicotine-induced suppression of conditioned place preference (CPP) [5]. Place aversion caused by vannicline (subcutaneous injection, 2.5 mg/kg, 3 days) is reliant on α5 nAChR but not β2 nAChR [5]. Subcutaneous injection of vannicline (0.1 and 0.5 mg/kg, 3 days) restores the somatic symptoms and hyperalgesia associated with nicotine withdrawal, as well as withdrawal-induced aversion, in a dose-related way [5].
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| Cell Assay |
Cell proliferation assay [1]
Cell Types: RAW 264.7 mouse macrophages (treated with 4 μg/mL LPS for 24 h) Tested Concentrations: 1 μM Incubation Duration: 0-48 h Experimental Results: LPS-induced cell proliferation rate diminished. Western Blot Analysis[4] Cell Types: HUVEC Tested Concentrations: 1, 10, 100 μM Incubation Duration: 24 hrs (hours) or 30 minutes Experimental Results: diminished VE-cadherin protein expression, activation of ERK1/2, p38 and JNK signaling. |
| Animal Protocol |
Animal/Disease Models: ICR male mice [5]
Doses: 0.01-1 mg/kg, 3 days Route of Administration: subcutaneous injection Experimental Results: Inhibited nicotine conditioned place preference (CPP) in a dose-dependent manner. |
| References |
[1]. Elif Baris, et al. Varenicline Prevents LPS-Induced Inflammatory Response via Nicotinic Acetylcholine Receptors in RAW 264.7 Macrophages. Front Mol Biosci. 2021 Oct 12;8:721533.
[2]. Mihalak KB, et al. Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors.Mol Pharmacol. 2006 Sep;70(3):801-5. Epub 2006 Jun 9. [3]. Jin H, et al. Therapeutic concentrations of varenicline in the presence of nicotine increase action potential firing in human adrenal chromaffin cells. J Neurochem. 2017 Jan;140(1):37-52. [4]. Mitsuhisa Koga, et al. Varenicline promotes endothelial cell migration by lowering vascular endothelial-cadherin levels via the activated α7 nicotinic acetylcholine receptor-mitogen activated protein kinase axis. Toxicology. 2017 Sep 1;390:1-9. [5]. Bagdas D, et al. New insights on the effects of varenicline on nicotine reward, withdrawal and hyperalgesia in mice.Neuropharmacology. 2018 Aug;138:72-79. |
| Molecular Formula |
C13H13N3
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| Molecular Weight |
211.26
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| CAS # |
249296-44-4
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| Related CAS # |
Varenicline dihydrochloride;866823-63-4;Varenicline Hydrochloride;230615-23-3;Varenicline Tartrate;375815-87-5;Varenicline-d4;2183239-01-0
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| SMILES |
C12=C(C=C3N=CC=NC3=C2)C4CC1CNC4
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| Synonyms |
CP 526555; CP-526555; CP526555; CP-526555-18; CP 526555 18; CP52655518; Varenicline tartrate; Chantix; Champix
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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) |
DMSO : ~20 mg/mL (~94.67 mM)
H2O : ≥ 20 mg/mL (~94.67 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.83 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 25.0 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: ≥ 2.5 mg/mL (11.83 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 25.0 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (11.83 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.7335 mL | 23.6675 mL | 47.3350 mL | |
| 5 mM | 0.9467 mL | 4.7335 mL | 9.4670 mL | |
| 10 mM | 0.4734 mL | 2.3668 mL | 4.7335 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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