Varenicline tartrate

Pricing Availability Delivery Time Qty
Cat.No. 3754 - Varenicline tartrate | C13H13N3.C4H6O6 | CAS No. 375815-87-5
Description: Orally active, subtype-selective α4β2 partial agonist
Chemical Name: 7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine tartrate
Purity: ≥99% (HPLC)
Datasheet
Citations (2)
Literature

Biological Activity

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.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

M. Wt 361.37
Formula C13H13N3.C4H6O6
Storage Desiccate at RT
Purity ≥99% (HPLC)
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 18.07 50
water 36.14 100

Preparing Stock Solutions

The following data is based on the product molecular weight 361.37. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Coe et al (2005) Varenicline: an α4β2 nicotinic receptor partial agonist for smoking cessation. J.Med.Chem. 48 3474 PMID: 15887955

Rollema et al (2007) Pharmacological profile of the α4β2 nicotinic acetylcholine receptor partial agonist varenicline, an effective smoking cessation aid. Neuropharmacology 52 985 PMID: 17157884

Rollema et al (2009) Preclinical pharmacology of the α4β2 nAChR partial agonist varenicline related to effects on reward, mood and cognition. Biochem.Pharmacol. 78 813 PMID: 19501054


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Keywords: Varenicline tartrate, supplier, nicotinic, receptors, subtype, selective, alpha4beta2, a4b2, α4β2, orally, active, nAChRs, acetylcholine, cholinergics, neuronal, nicotine, Pfizer, Nicotinic, (a4b2), Receptors, Tocris Bioscience

2 Citations for Varenicline tartrate

Citations are publications that use Tocris products. Selected citations for Varenicline tartrate include:

Kuryatov et al (2013) Chemical chaperones exceed the chaperone effects of RIC-3 in promoting assembly of functional α7 AChRs. Sci Rep 8 e62246 PMID: 23638015

Price et al (2015) Varenicline Interactions at the 5-HT3 Receptor Ligand Binding Site are Revealed by 5-HTBP. PLoS One 6 1151 PMID: 25648658


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