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SR 33805 oxalate

A Specific Blocker of L-Type CaV Channels

Cat #: S-105
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 654.77
    Purity: >96%
    Effective concentration 1 nM - 10 μM.
    Structure
    Chemical name 3,4-Dimethoxy-N-methyl-N-[3-[4-[[1-methyl-3-(1-methylethyl)-1H-indol-2-yl]sulfonyl]phenoxy]propyl]benzeneethanamine oxalate.
    Molecular formula C32H40N2O5S.C2H2O4.
    CAS No.: 121346-32-5
    Activity SR 33805, a fantofarone derivative, is a potent Ca2+ channel antagonist1. It binds allosterically to the α1-subunit of L-type Ca2+ channels (Kd = 20 pM), at a site distinct from other types of blockers2. It potently inhibits the Ca2+ channel in primary mouse cardiac myocytes cultures with IC50 values ranging from 4 to 33 nM3.
    References-Activity
    1. Cazorla, O. et al. (2003) Br. J. Pharmacol. 139, 99.
    2. Chatelain, P. et al. (1994) Eur. J. Pharmacol. 267, 151.
    3. Romey, G. et al. (1994) Eur. J. Pharmacol. 263, 101.
    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 SR 33805 oxalate blocks L-type Ca2+ currents in Xenopus oocytes.
      Alomone Labs SR 33805 oxalate 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 μM SR 33805 oxalate (#S-105) as indicated, and upon wash. Holding potential was -80 mV and currents were elicited every 10 seconds by 100 ms ramp to +60 mV. B. Superimposed current traces of L-type currents before and during applications of 1 μM SR 33805 oxalate, taken from the experiment 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. Cazorla, O. et al. (2003) Br. J. Pharmacol. 139, 99.
    4. Chatelain, P. et al. (1994) Eur. J. Pharmacol. 267, 151.
    5. Romey, G. et al. (1994) Eur. J. Pharmacol. 263, 101.
    6. Chatelain, P. et al. (1993) Eur. J. Pharmacol. 246, 181.
    7. Magnier-Gaubil, C. et al. (1996) J. Biol. Chem. 271, 27788.
    Scientific background

    Two types of voltage-gated Ca2+ channels (VGCC, CaV) are found in most nonexcitable cells, T-type and the L-type Ca2+ channels1-2.

    SR 33805, a fantofarone derivative, is a potent Ca2+ channel antagonist3. It binds allosterically to the a1-subunit of L-type Ca2+ channels (Kd = 20 pM), at a site distinct from other types of blockers4. It potently inhibits the Ca2+ channel, and hence prevents Ca2+ influx, in primary mouse cardiac myocytes cultures with IC50 values ranging from 4.1 to 33 nM5.

    SR 33805 shows selectivity for vascular smooth muscle, inducing vasorelaxation without producing inotropic or chronotropic effects6. It inhibits PDGF-stimulated smooth muscle cell proliferation and the associated rise in intracellular Ca2+ concentration with IC50 values of 0.2 µM and 0.3 µM, respectively7.

    Despite its strong Ca2+-antagonistic properties, SR33805 increases cardiac cell contractile activity as a consequence of its Ca2+-sensitizing effects. These effects are attributable to both an increase in the maximal Ca2+-activated force and a length-dependent Ca2+-sensitization3.

    Target L-type Ca2+ channels
    Last update: 12/08/2021

    SR 33805 oxalate (#S-105) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use

    Applications

    Specifications

    Scientific Background

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