Varenicline Hydrochloride
Based on 1 Customer Validation
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 α6β2 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: 99.94%
- CAS No.: 230615-23-3
- Formula: C13H14ClN3
- Molecular Weight:247.72
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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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Biological Activity
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.
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Animal Model:Eighty male Wistar rats (250-300 g)[1]
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Dosage:0.5 mg/kg/day, 1 mg/kg/day or 2 mg/kg/day
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Administration:Subcutaneous injection; twice daily; for 14 days
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Result:Significantly higher DRD2/3 availability in the ventral striatum of approximately 11%, while only the rats treated with 1 and 2 mg/kg/day dose showed significantly higher DRD2/3 availability in the dorsal striatum by 12.5% and 13.2%, respectively.
Chemical Information
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CAS No. 230615-23-3
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Appearance Solid
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Molecular Weight 247.72
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Formula C13H14ClN3
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Color Light yellow to khaki
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SMILES
C1(C2CC3CNC2)=C3C=C(N=CC=N4)C4=C1.Cl
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Synonyms
CP 526555 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H2O : 50 mg/mL (201.84 mM; Need ultrasonic)
DMSO : ≥ 2.5 mg/mL (10.09 mM; 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* 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)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 100 mg/mL (403.68 mM); Clear solution; Need ultrasonic
Purity & Documentation
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Data Sheet (282 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)
- Korean - KR (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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 4.0368 mL | 20.1841 mL | 40.3682 mL | 100.9204 mL |
| 5 mM | 0.8074 mL | 4.0368 mL | 8.0736 mL | 20.1841 mL | |
| 10 mM | 0.4037 mL | 2.0184 mL | 4.0368 mL | 10.0920 mL | |
| H2O | 15 mM | 0.2691 mL | 1.3456 mL | 2.6912 mL | 6.7280 mL |
| 20 mM | 0.2018 mL | 1.0092 mL | 2.0184 mL | 5.0460 mL | |
| 25 mM | 0.1615 mL | 0.8074 mL | 1.6147 mL | 4.0368 mL | |
| 30 mM | 0.1346 mL | 0.6728 mL | 1.3456 mL | 3.3640 mL | |
| 40 mM | 0.1009 mL | 0.5046 mL | 1.0092 mL | 2.5230 mL | |
| 50 mM | 0.0807 mL | 0.4037 mL | 0.8074 mL | 2.0184 mL | |
| 60 mM | 0.0673 mL | 0.3364 mL | 0.6728 mL | 1.6820 mL | |
| 80 mM | 0.0505 mL | 0.2523 mL | 0.5046 mL | 1.2615 mL | |
| 100 mM | 0.0404 mL | 0.2018 mL | 0.4037 mL | 1.0092 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.
Varenicline Hydrochloride Related Classifications
HY-10020 Related Classifications
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