Varenicline tartrate
Tocris Bioscience, part of Bio-Techne | Catalog # 3754
Selective α4β2 nAChR partial agonist; orally active
Key Product Details
Description
Selective α4β2 nAChR partial agonist; orally active
Product Description
Varenicline tartrate is an orally active, subtype-selective partial agonist at α4β2 nicotinic receptors (Ki values are 0.06, 240, 322 and 3540 nM for α4β2, α3β4, α7, α1βγδ receptors respectively). Reduces nicotine-evoked dopamine release in vitro and decreases nicotine self-administration in vivo. Also potently activates PSAM4-5-HT3 and PSAM4-GlyR chimeric ion channels (EC50 values are 4 and 1.6 nM, respectively)Licensing Information
Sold for research purposes under agreement from Pfizer Inc.Product Specifications
Molecular Weight
361.37
Formula
C13H13N3.C4H6O6
Storage
Desiccate at RT
Purity
≥99% (HPLC)
Chemical Name
7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine tartrate
CAS Number
375815-87-5
PubChem ID
5310966
InChI Key
JQSHBVHOMNKWFT-DTORHVGOSA-N
SMILES
OC(C(O)C(O)=O)C(O)=O.C1(C=C([C@H]4CNC[C@@H]3C4)C3=C2)=C2N=CC=N1
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 36.14 | 100 | |
| DMSO | 18.07 | 50 |
Preparing Stock Solutions
for Varenicline tartrate
The following data is based on the product molecular weight 361.37
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.77 mL | 13.84 mL | 27.67 mL |
| 5 mM | 0.55 mL | 2.77 mL | 5.53 mL |
| 10 mM | 0.28 mL | 1.38 mL | 2.77 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.55 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Rollema Pharmacological profile of the α4β2 nicotinic acetylcholine receptor partial agonist varenicline, an effective smoking cessation aid. Neuropharmacology 2007 PMID: 17157884
- Rollema Preclinical pharmacology of the α4β2 nAChR partial agonist vareni. related to effects on reward, mood and cognition. Biochem.Pharmacol. 2009 PMID: 19501054
- Coe Varenicline: an α4β2 nicotinic receptor partial agonist for smoking cessation. J.Med.Chem. 2005 PMID: 15887955
Product Specific Notices for Varenicline tartrate
For research use only
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