Varenicline
Based on 1 publication(s) in Google Scholar
Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α7β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation.
For research use only. We do not sell to patients.
- Purity: 99.92%
- CAS No.: 249296-44-4
- Formula: C13H13N3
- Molecular Weight:211.27
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Varenicline
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Biological Activity
EC50: 2.3 μM (α4β2 nAChR); 18 μM (α7 nAChR); 55 μM (α3β4 nAChR)[1]
Varenicline (200 μM, 24 h) shows no affection to cell viability of HUVEC cells[3].
Varenicline (100 μM, 24 h) lowers expression of VE-cadherin in HUVEC cells as Varenicline (100 μM, 30 min) significantly activates ERK1/2 and p38 signaling[3].
Varenicline (100 μM, 4 h) promotes migration of HUVEC cells by 2.4-fold[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HUVEC
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Concentration:100, 200, 300, 500 μM
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Incubation Time:24 h
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Result:Did not affect cell viability at 100 and 200 μM (96.8 ± 0.1% and 93.9 ± 1.8%, respectively). Decreased cell viability to 85.7 ± 7.5% and 57.8 ± 7.7% for 300 and 500 μM, respectively.
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Cell Line:HUVEC
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Concentration:100 μM
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Incubation Time:1, 5, 10, 15 ,30 ,60 min, 24 h
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Result:Significantly activated ERK1/2 and p38 signaling with peak activity at 10–15 min and 10–30 min after treatment, respectively, lowered expression of VE-cadherin at 24 h. MLA (100 nM) significantly reversed the Varenicline-induced effects.
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Cell Line:HUVEC
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Concentration:100 μM
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Incubation Time:4 h
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Result:Significantly increased the number of migrating cells by 2.4-fold compared with vehicle treatment. MLA (100 nM) completely blocked Varenicline-stimulated migration.
Varenicline (0.004–0.04 mg/kg/h, i.v.drip, 23h a day for 7-10 d) dose-dependently reduces self-administration of nicotine alone (0.0032 mg/kg/inj), and in combination with cocaine (0.0032 mg/kg/inj) with no significant effects on food-maintained responding in cocaine- and nicotine-experienced adult rhesus monkeys[5].
Varenicline (0.178-5.6 mg/kg, i.p., acute administration) shows antidepressant-like activity in the forced swim test in C57BL/6J and CD-1 mice[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 249296-44-4
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Appearance Solid
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Molecular Weight 211.27
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Formula C13H13N3
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Color Light yellow to yellow
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SMILES
C12=C(C=C3N=CC=NC3=C2)C4CC1CNC4
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Synonyms
CP 526555
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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FASEB J
2025 Nov 30;39(22):e71247. PMID: 41269536
Solvent & Solubility
H2O : ≥ 20 mg/mL (94.67 mM)
DMSO : 20 mg/mL (94.67 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (11.83 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (11.83 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Koegelenberg CF, et al. Efficacy of varenicline combined with nicotine replacement therapy vs varenicline alone for smoking cessation: a randomized clinical trial. JAMA. 2014 Jul;312(2):155-61. [Content Brief]
[2]. Magnus CJ, et al. Ultrapotent chemogenetics for research and potential clinical applications. Science. 2019;364(6436):eaav5282. [Content Brief]
[3]. Koga M, 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;390:1-9. [Content Brief]
[4]. Ren J, et al. Countering Opioid-induced Respiratory Depression in Male Rats with Nicotinic Acetylcholine Receptor Partial Agonists Varenicline and ABT 594. Anesthesiology. 2020 May;132(5):1197-1211. [Content Brief]
[5]. Mello NK, et al. Effects of chronic varenicline treatment on nicotine, cocaine, and concurrent nicotine+cocaine self-administration. Neuropsychopharmacology. 2014 Apr;39(5):1222-31. [Content Brief]
[6]. Rollema H, et al. Varenicline has antidepressant-like activity in the forced swim test and augments sertraline's effect. Eur J Pharmacol. 2009 Mar 1;605(1-3):114-6. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 4.7333 mL | 23.6666 mL | 47.3332 mL | 118.3331 mL |
| 5 mM | 0.9467 mL | 4.7333 mL | 9.4666 mL | 23.6666 mL | |
| 10 mM | 0.4733 mL | 2.3667 mL | 4.7333 mL | 11.8333 mL | |
| 15 mM | 0.3156 mL | 1.5778 mL | 3.1555 mL | 7.8889 mL | |
| 20 mM | 0.2367 mL | 1.1833 mL | 2.3667 mL | 5.9167 mL | |
| 25 mM | 0.1893 mL | 0.9467 mL | 1.8933 mL | 4.7333 mL | |
| 30 mM | 0.1578 mL | 0.7889 mL | 1.5778 mL | 3.9444 mL | |
| 40 mM | 0.1183 mL | 0.5917 mL | 1.1833 mL | 2.9583 mL | |
| 50 mM | 0.0947 mL | 0.4733 mL | 0.9467 mL | 2.3667 mL | |
| 60 mM | 0.0789 mL | 0.3944 mL | 0.7889 mL | 1.9722 mL | |
| 80 mM | 0.0592 mL | 0.2958 mL | 0.5917 mL | 1.4792 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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