TTA-A2

A Blocker of T-Type CaV Channels
    Cat #: T-140
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 378.39
    Purity: >99%
    Form Lyophilized powder.
    Effective concentration 0.05-100 µM.
      • TTA-A2
    Chemical name (R)-2-(4-cyclopropylphenyl)-N-(1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl) acetamide.
    Molecular formula C20H21F3N2O2.
    CAS No.: 953778-63-7
    Activity TTA-A2 blocks T-type CaV channels with an IC50 of ~100 nM (at -100 mV holding potential) and ~5 µM (at holding potential -80 mV).
      • Kraus, R.L. et al. (2010) J. Pharmacol. Exp. Ther. 335, 409.
    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 100mM in DMSO. Centrifuge all product preparations before use (10000 x g for 1 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
      • TTA-A2
        Alomone Labs TTA-A2 blocks T-type CaV channels expressed in Xenopus oocytes.
        A. Time course of CaV3.2 peak current amplitude, elicited by 100 ms voltage step from holding potential of -100 mV to -30 mV, delivered every 10 seconds. Application of 100 µM TTA-A2 (#T-140) inhibits the CaV3.2 current in a reversible manner (indicated by the horizontal bar). B. Representative current traces before and during application of 100 µM TTA-A2 as indicated.
        TTA-A2
        Alomone Labs TTA-A2 blocks T-type CaV channels expressed in Xenopus oocytes.
        A. Time course of CaV3.1 peak current amplitude, elicited by 50 ms voltage step from holding potential of -80 mV to -20 mV, delivered every 10 seconds. Application of 1 µM TTA-A2 (#T-140) inhibits the CaV3.1 current in a reversible manner (indicated by the horizontal bar). B. Representative current traces before and during application of 1 µM TTA-A2 as indicated.
    References - Scientific background
    • 1. Giordanetto, F. et al.  (2011) Expert Opin. Ther. Pat. 21, 85.
    • 2. Reger, T.S. et al. (2011) Bioorg. Med. Chem. Lett. 21, 1692.
    • 3. Kraus, R.L. et al. (2010) J. Pharmacol. Exp. Ther. 335, 409.
    • 4. Uebele, V.N. et al. (2009) Cell. Biochem. Biophys. 55, 81.
    • 5. Francois, A. et al.  (2013) Pain 154, 283.
    • 6. Uslaner, J.M. et al. (2010) Biol. Psychiatry 68, 712.
    • 7. Uebele, V.N. et al. (2009) J. Clin. Invest. 119, 1659.
    • 8. Uslaner, J.M. et al. (2012) Neuropharmacology 62, 1413.
      • Low-voltage-activated (T-type/CaV3) Ca2+ channels are a subclass of voltage-dependent Ca2+ channels allowing Ca2+ entry near the resting potential of most cells1. Various synthetic T-channel blockers have been described in the past few years including TTA-A2, a potent, state-dependent, and highly selective T-type CaV antagonist2.

        TTA-A2 was found to inhibit all three subtypes of low-voltage-gated T-type channels (CaV3.1, CaV3.2, and CaV3.3) with comparable potencies. Changing membrane resting potentials from −100 to −80 mV enhanced compound potency ∼40-fold, from an IC50 of ∼4 μM to 0.1 μM, respectively, indicating state dependence of inhibition3. in vivo studies have demonstrated that TTA-A2 reduces absence epilepsy seizures4, pain perception5, nicotine self-administration6 and weight gain7. It also improves the quality of sleep7 and displays antipsychotic properties8.

    Target T-type CaV channels
    Image & Title TTA-A2
    Alomone Labs TTA-A2 inhibits T-type CaV channels in response to hypoxia.Representative example of sensory nerve response (impulses (imp)/s) to hypoxia in the presence of vehicle or 25 μM TTA-A2 (#T-140), and 5 min after washout (left panel). Effect of TTA-A2 on sensory nerve response to hypoxia (right panel).Adapted from Makarenko, V.V. et al. (2015) Am. J. Physiol. 308, C146. with permission of the American Physiological Society.
    Last update: 23/09/2019

    TTA-A2 (#T-140) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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