Varenicline tartrate

CP-526,555, Chantix®, Champix®
A Partial Agonist of α4/β2 nAChR and a Full Agonist of α7 nAChR
    Cat #: V-105
    Alternative Name CP-526,555, Chantix®, Champix®
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 361.3
    Purity: >99% (HPLC)
    Effective concentration 1-100 μM.
    Structure
    • Varenicline tartrate
    Chemical name 7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine tartrate.
    Molecular formula C13H13N3*C4H6O6.
    CAS No.: 375815-87-5.
    Activity Varenicline tartrate is a partial agonist of α4/β2 nicotinic acetylcholine receptors and a full agonist of α7 nAChR1, and may be suitable for treating nicotine addiction2.
    References-Activity
    1. Mihalak, K.B. et al. (2006) Mol. Pharmacol. 70, 801.
    2. De Biasi, M. and Salas, R. (2008) Exp. Biol. Med. 233, 917.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility Any aqueous buffer. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to one week at 4°C or six months at -20°C.
    Our bioassay
    • Varenicline tartrate
      Alomone Labs Varenicline tartrate activates α7 nicotinic acetylcholine receptor channels heterologously expressed in Xenopus oocytes.
      Current traces of α7 nicotinic acetylcholine receptor channels activity at -60 mV holding potential. 100 μM Varenicline tartrate (#V-105) alone activates a transient relatively small current (right), while perfusing PNU-120596 prior to Varenicline tartrate activates a much larger current (left), even at a 10 fold lower concentration (middle). Periods of compound perfusion are indicated by the horizontal bars: PNU; PNU-120596, VAR; Varenicline tartrate.
    References - Scientific background
    1. Mihalak, K.B. et al. (2006) Mol. Pharmacol. 70, 801.
    2. Rollema, H. et al. (2007) Neuropharmacology 52, 985.
    3. Papke, R.L. et al. (2010) J. Pharmacol. Exp.Ther. 333, 501.
    4. De Biasi, M. and Salas, R. (2008) Exp. Biol. Med. 233, 917.
    5. Nides, M. et al. (2006) Arch. Intern. Med. 166, 1561.
    6. Foulds, J. (2006) Int. J. Clin. Pract. 60, 571.
    Scientific background

    Varenicline tartrate is a partial agonist of α4/β2 nicotinic Acetylcholine receptors (nAChR) and a full agonist of a7 nAChR1, it is also an effective activator of α3/β4 receptors with apparent EC50 in the mM range2,3. Based on these characteristics, especially the partial agonistic activity towards the α4/β2 nAChR, it may be suitable for treating nicotine addiction4-6.

    In vitro functional patch clamp studies in HEK cells expressing nAChRs show that varenicline is a partial agonist with 45% of nicotine's maximal efficacy at α4/β2 nAChRs and inhibited the nicotine induced currents2. In addition, varenicline reduced nicotine self-administration in rats2.

    Target α4/β2, α7 nAChR
    Last update: 24/01/2020

    Varenicline tartrate (#V-105) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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