L-651,582

Carboxyamidotriazole
An Effective Blocker of L-Type CaV Channels
    Cat #: L-110
    Alternative Name Carboxyamidotriazole
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 424.7
    Purity: >99%
    Effective concentration 0.5-200 μM.
      • L-651,582
    Chemical name 5-Amino-1-[[3,5-dichloro-4-(4-chlorobenzoyl)phenyl]methyl]-1H-1,2,3-triazole-4-carboxamide.
    Molecular formula C17H12Cl3N5O2.
    CAS No.: 99519-84-3.
    Activity L-651,582 inhibits CaV channels as well as receptor activated Ca2+ signals in guinea pig atrial cells1, thus it is an L-type, voltage-gated Ca2+ channel blocker with additional antiproliferative activities2.
      • Hupe, D.J. et al. (1991) J. Biol. Chem. 266, 10136.
      • Guo, L. et al. (1991) Eur. J. Pharmacol. 538, 15.
    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 DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
      • L-651,582
        Alomone Labs L-651,582 blocks L-type Ca2+ currents in Xenopus oocytes.
        A. Time course of L-type channel (CaV1.2+α2δ11a) activity before and during applications of 1, 10 and 100 μM L-651,582 (#L-110) and upon wash. Holding potential was -100 mV and currents were elicited every 10 seconds by 100 ms steps to 0 mV. Periods of compound application are indicated by symbols in the inset. B. Example of superimposed current traces before and during application of 1, 10 and 100 μM L-651,582 (taken from the experiment described in A).
    References - Scientific background
    • 1. Schramm, M. et al. (1988) Calcium in drug actions (Baker, P. F., ed), 90-113.
    • 2. Narahashi, T. et al. (1988) Calcium in drug actions (Baker, P. F., ed), 255-174.
    • 3. Kohn, E.C. et al. (1990) J. Nat. Cancer Int82, 54.
    • 4. Felder, C.C. et al.(1991) J. Pharm. Exp. Ther257, 967.
    • 5. Hupe, D.J. et al. (1991) J. Biol. Chem. 266, 10136.
    • 6. Yang, J.L. et al. (2008) Int. J. Cancer 123, 258.
      • Two subtypes of voltage-gated Ca2+ channels (VGCC, CaV) are found in most non-excitable cells, the T-type (CaV3) and the L-Type (CaV1) Ca2+ channels1-2.

        L-651,582 is an anti-proliferative, anti-angiogenic, anti-metastatic and anti-parasitic agent3-5, which is also selective towards numerous mismatch repair-deficient tumor cell lines in vitro.6 It is a voltage-gated L-type Ca2+ channel blocker with an IC50 of 0.5 µg/ml5 . Patch clamp measurements of current through L- and T-type channels in guinea pig atrial cells also indicate that L-651,582 is a Ca2+ antagonist5. Block of L-type Ca2+ channels is voltage-dependent and the apparent dissociation constant for the high affinity state is 0.2 µg/ml. The IC50 for block of T-type Ca2+ channels is 1.4 µg/ml5.

    Target L-type Ca2+ channels
    Last update: 24/01/2020

    L-651,582 (#L-110) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use