FPL 64176

An Opener of L-type Ca2+ Channels
    Cat #: F-160
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 347.4
    Purity: >99% (HPLC)
    Form Lyophilized powder.
    Effective concentration 10 nM - 1 µM.
      • FPL 64176
    Chemical name methyl 4-(2-benzylbenzoyl)-2,5-dimethyl-1H-pyrrole-3-carboxylate.
    Molecular formula C22H21NO3.
    CAS No.: 120934-96-5.
    PubChem CID 3423
    Activity FPL 64176 is an L-type Ca2+ channel activator, which induces contraction in rat tail artery1.
      • Zheng, W. et al. (1991) Mol. Pharmacol. 40, 734.
    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 100 mM in DMSO. Centrifuge all product preparations before use (10 000 x g for 1 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
      • FPL 64176
        Alomone Labs FPL 64176 increases L-type CaV channels currents expressed in Xenopus oocytes.
        A. Time course of CaV1.2 (co expressed with α2δ1 and β1 auxiliary subunits) tail peak current amplitude, elicited by 100 ms voltage step from holding potential of -100 mV to -10 mV, delivered every 10 seconds. Application of 0.1 and 1 µM FPL 64176 (#F-160) increases the CaV1.2 current (indicated by the horizontal bar). B. Representative current traces before and during application of 0.1 and 1 µM FPL 64176 (as indicated).
    References - Scientific background
    • 1. Zheng, W. et al. (1991) Mol. Pharmacol. 40, 734.
    • 2. Ghais, N.S. et al. (2009) Exp. Physiol. 94, 240.
    • 3. McDonough, S.I. et al. (2005) Biophys. J. 88, 211.
    • 4. Fan, J.S. et al. (2002) Br. J. Pharmacol. 135, 1495.
    • 5. Catterall, W.Aet al. (2003) Pharmacol. Rev. 55, 579.
      • FPL 64176 acts as a non-dihydropyridine L-type calcium channel activator with high efficacy properties. It's a benzoylpyrrole compound that has the ability to increase macroscopic inward current through L-type calcium channels. It extends the opening of single calcium channels during depolarization and slows channel closing upon repolarization without affecting currents through other calcium channels1-3.

        FPL 64176 is being used as a tool for studying the physiological roles and disorders of L-type channels, identification of L-type currents within the mix of channel subtypes and for increasing the contractility of smooth and cardiac muscle2.

        The use of FPL 64176 has revealed an inactivation and adaptation process for ryanodine receptors and the presence of cardiac sparklets3,4.

        L-type voltage-gated calcium channels are one of the three major classes (CaV1-CaV3) of voltage-gated calcium channels. They are expressed in many excitable tissues and play as important transducers in the plasma membrane, altering membrane depolarization to intracellular signaling. Many physiological functions, including brain, endocrine, and sensory functions and muscle contraction rely on proper L-type channel activity5.

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

    FPL 64176 (#F-160) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use