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L-651,582

Carboxyamidotriazole

An Effective Blocker of L-Type CaV Channels

Cat #: L-110
Alternative Name Carboxyamidotriazole
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 424.7
    Purity: >99%
    Effective concentration 0.5-200 μM.
    Structure
    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.
    References-Activity
    1. Hupe, D.J. et al. (1991) J. Biol. Chem. 266, 10136.
    2. 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.
    Our bioassay
    • Alomone Labs L-651,582 blocks L-type Ca2+ currents in Xenopus oocytes.
      Alomone Labs L-651,582 blocks L-type Ca2+ currents in Xenopus oocytes.
      A. Time course of L-type channel (CaV1.2+α2δ1+β1a) 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 Int. 82, 54.
    4. Felder, C.C. et al.(1991) J. Pharm. Exp. Ther. 257, 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.
    Scientific background

    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
    Lyophilized Powder
    Last update: 24/01/2021

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

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    For research purposes only, not for human use

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    L-Type (CaV1) Channels

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