TTA-P2

A Blocker of T-type CaV Channels
    Cat #: T-155
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 431
    Purity: >96% (HPLC)
    Formulation Lyophilized powder.
    Effective concentration 0.05-10 µM.
    Structure
    Chemical name 3,5-dichloro-N-[1-(2,2-dimethyl-tetrahydro-pyran-4-ylmethyl)-4-fluoro-piperidin-4-ylmethyl]-benzamide. Racemic mixture.
    Molecular formula C21H29Cl2FN2O2.
    CAS No.: 918430-49-6, 1072018-68-8.
    Activity TTA-P2 blocks T-type currents in DRGs with IC50 of 100 nM and 22 nM in thalamocortical and reticular neurons1,2.
    References - Activity
    1. Choe, W. et al. (2011) Mol. Pharmacol. 80, 900.

    2. Dreyfus, F.M. et al. (2010) J. Neurosci. 30, 99.

    Storage before reconstitution 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.
    Reconstitution Up to 25mM in DMSO. Centrifuge all product preparations before use (10000 x g for 1 min).
    Storage after reconstitution Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    Alomone Labs TTA-P2 inhibits T-type CaV channels heterologously expressed in Xenopus oocytes.
    A. Time course of CaV3.2 peak current amplitude, elicited by 100 ms voltage step from holding potential of -100mV to -30 mV, delivered every 10 seconds. Application of 5 µM TTA-P2 (#T-155) inhibits the CaV3.2 current in a reversible manner (indicated by the horizontal bar). B. Representative current traces before and during application of 5 µM TTA-P2 as indicated.
    References - Scientific Background
    1. Dreyfus, F.M. et al. (2010) J. Neurosci. 30, 99.
    2. Choe, W. et al. (2011) Mol. Pharmacol. 80, 900.
    Scientific background

    TTA-P2 is a novel, potent and selective T-type CaV blocker. In thalamocortical and reticular neurons, it blocks T-type currents with an IC50 of 22 nM without affecting high voltage Ca2+ channels1. In rat DRGs, it blocks T-type currents with an IC50 of 100 nM and stabilizes the channel in the inactive state2.

    TTA-P2 has the potential of acting as an antinociceptive agent2.

    Target T-type CaV channels
    Image & Title TTA-P2
    Alomone Labs TTA-P2 inhibits T-type CaV channels in AZF cells.Bovine adrenal zona fasciculate (AZF) whole cell recordings. Ca2+ currents were recorded in 10 mM Ba2+ in response to voltage steps to -5 mV, applied from a holding potential of -80 mV, before and after superfusion of the cell with 2 μM TTA-P2 (#T-155), (left panel). Concentration-dependent inhibition of CaV3.2 currents by TTA-P2. Values are means ± SE for number of determinations shown in parentheses (right panel).Adapted from Enyeart, J.J. and Enyeart, J.A. (2015) Am. J. Physiol. 308, C899. with permission of the American Physiological Society.
    Last update: 02/01/2019

    TTA-P2 (#T-155) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
    Citations
    Product citations
    1. Chen, W. et al. (2018) Front. Mol. Neurosci. 11, 24.
    2. Stamenic, T.T. and Todorovic, S.M. (2018) eNeuro 5, e0016.
    3. Tracy, M.E. et al. (2018) Neuropharmacology 135, 343.
    4. Huang, C.Y. et al. (2017) J. Neurosci. 37, 4433.
    5. Irie, T. and Trussell, L.O. (2017) Neuron 96, 856.

    6. Kisiswa, L. et al. (2017) Open Biol. 7, 160288.
    7. Lu, J.M. et al. (2017) Cereb. Cortex 27, 3842.
    8. Yang, C. et al. (2017) Neuroscience 352, 249.
    9. Zhao, Y. et al. (2017) Neuron 96, 355.
    10. Barzan, R. et al. (2016) Front. Cell. Neurosci. 10, 135.
    11. Kortus, S. et al. (2016) Cell Calcium 59, 289.
    12. Moutal, A. et al. (2016) Pain 157, 1448.
    13. Xie, J.Y. et al. (2016) Pain 157, 2124.
    14. Yang, T. et al. (2016) Hypertension 68, 785.
    15. Enyeart, J.J. et al. (2015) Am. J. Physiol. Cell Physiol. 308, C899.
    16. Rivera-Arconada, I and Lopez-Garcia, J.A. (2015) Pflugers Arch. 467, 1985.
    17. Scott, A.L. et al. (2015) J. Physiol. 593, 3281.
    18. Seol, M. and Kuner, T. (2015) Eur. J. Neurosci. 42, 3033.
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