Varenicline Tartrate (Synonyms: CP 526,55518) |
Catalog No.GC10948
One-Click Copy Product Info
|
Varenicline Tartrate is a selective α7 and α4β2 nicotinic acetylcholine receptor (nAChR) agonist with an IC50 value of 250nM for α4β2 nAChR.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 375815-87-5
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
Varenicline Tartrate is a selective α7 and α4β2 nicotinic acetylcholine receptor (nAChR) agonist with an IC50 value of 250nM for α4β2 nAChR[1]. Varenicline Tartrate is a smoking cessation drug that can reduce nicotine dependence[2, 3].
In vitro, Varenicline Tartrate (1, 10, 100μM) treatment of human umbilical vein endothelial cells (HUVEC) for 24h reduced the expression of VE-cadherin in cells and promoted cell migration[4].
In vivo, Varenicline Tartrate (0.25-1.5mg/kg, 0.178-5.6mg/kg) was intraperitoneally injected into C57BL/6J and CD-1 mice, respectively, and showed antidepressant-like activity in the forced swimming test of mice, significantly reducing the immobility of both mice[5].
References:
[1] Magnus C J, Lee P H, Bonaventura J, et al. Ultrapotent chemogenetics for research and potential clinical applications[J]. Science, 2019, 364(6436): eaav5282.
[2] Fagerström K, Hughes J. Varenicline in the treatment of tobacco dependence[J]. Neuropsychiatric Disease and Treatment, 2008, 4(2): 353-363.
[3] Faessel H M, Obach R S, Rollema H, et al. A review of the clinical pharmacokinetics and pharmacodynamics of varenicline for smoking cessation[J]. Clinical pharmacokinetics, 2010, 49(12): 799-816.
[4] Koga M, Kanaoka Y, Sugiyama K, 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[J]. Toxicology, 2017, 390: 1-9.
[5] Rollema H, Guanowsky V, Mineur Y S, et al. Varenicline has antidepressant-like activity in the forced swim test and augments sertraline's effect[J]. European Journal of Pharmacology, 2009, 605(1-3): 114-116.
| Cell experiment [1]: | |
Cell lines | Human umbilical vein endothelial cells (HUVECs) |
Preparation Method | Cells were treated with Varenicline Tartrate (1, 10, and 100μM) for 24h, and then the expression of VE-cadherin was detected. |
Reaction Conditions | 1, 10, 100μM; 24h |
Applications | Varenicline Tartrate lowers expression of VE-cadherin in HUVECs. |
| Animal experiment [2]: | |
Animal models | C57BL/6J mice、CD-1 mice |
Preparation Method | C57BL/6J mice were treated with vehicle and Varenicline Tartrate (0.25-1.5mg/kg, i.p.). CD-1 mice were treated with vehicle, amitriptyline (10mg/kg), and Varenicline Tartrate (0.178-5.6mg/kg). The immobility time and activity time of mice were recorded every 30s for 5min and expressed as mean swimming time ± SEM. |
Dosage form | 0.25-1.5mg/kg、0.178-5.6mg/kg; i.p. |
Applications | Varenicline Tartrate significantly reduced immobility in both mouse strains. |
References: | |
| Cas No. | 375815-87-5 | SDF | |
| Synonyms | CP 526,55518 | ||
| Chemical Name | (6R)-7,8,9,10-tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline (2R,3R)-2,3-dihydroxysuccinate | ||
| Canonical SMILES | O=C([C@]([C@@](C(O[H])=O)([H])O[H])([H])O[H])O[H].[H][C@@]12C([H])([H])C(C([H])([H])N([H])C2([H])[H])([H])C3=C([H])C4=NC([H])=C([H])N=C4C([H])=C13 | ||
| Formula | C13H13N3.C4H6O6 | M.Wt | 361.35 |
| Solubility | ≥ 18.07mg/mL in DMSO, ≥ 96.2 mg/mL in Water | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.7674 mL | 13.837 mL | 27.674 mL |
| 5 mM | 553.5 μL | 2.7674 mL | 5.5348 mL |
| 10 mM | 276.7 μL | 1.3837 mL | 2.7674 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)