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TTA-A2

A Blocker of T-Type CaV Channels

Cat #: T-140
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 378.39
    Purity: >99%
    Form Lyophilized powder.
    Effective concentration 0.05-100 µM.
    Structure
    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).
    References-Activity
    1. 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.
    Our bioassay
    • Alomone Labs TTA-A2 blocks T-type CaV channels expressed in Xenopus oocytes.
      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.
    • Alomone Labs TTA-A2 blocks T-type CaV channels expressed in Xenopus oocytes.
      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.
    Scientific background

    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
    Lyophilized Powder
    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: 02/01/2022

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

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    For research purposes only, not for human use

    Applications

    Citations

    Citations
    Product citations
    1. Drumm, B.T. et al. (2018) J. Physiol. 596, 1433.
    2. Hu, W. and Bean, B.P. (2018) Neuron 97, 1315.
    3. Nishizawa, Y. et al. (2018) J. Neurosci. Res. 96, 901.
    4. Stamenic, T.T. and Todorovic, S.M. (2018) eNeuro 5, e0016.
    5. Kisiswa, L. et al. (2017) Open Biol. 7, 160288.
    6. Resch, J.M. et al. (2017) Neuron 96, 190.
    7. Sankhe, S. et al. (2017) Biochem. Biophys. Acta 1864, 1631.
    8. Makarenko, V.V. et al. (2016) J. Neurophysiol. 115, 345.
    9. Fernandez, J.A. et al. (2015) Invest. Ophtalmol. Vis. Sci. 56, 5125.
    10. Makarenko, V.V. et al. (2015) Am. J. Physiol. 308, C146.

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