PD 173212

A Novel Blocker of N-type CaV Channels
    Cat #: P-105
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 599.9
    Purity: >99%
    Effective concentration 10 nM - 10 μM.
      • PD 173212
    Chemical name N-[[4-(1,1-Dimethylethyl)phenyl]methyl-N-methyl-L-leucyl-N-(1,1-dimethylethyl)-O-phenylmethyl)-L-tyrosinamide.
    Molecular formula C38H53N3O3.
    CAS No.: 217171-01-2.
    Activity PD 173212 is a dipeptidyl-amine that acts as an N-type voltage-gated Ca2+ channel blocker1. PD 173212 inhibited N-type channels in IMR-32 cells with IC50 = 36 nM as measured by Ca2+ imaging of K+ stimulated cells and only had small effects on other channels at much higher concentrations1.
      • Hu, L.Y. et al. (1999) Bioorg. Med. Chem. Lett. 9, 2151.
    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.
      • PD 173212
        Alomone Labs PD 173212 blocks N-type Ca2+ currents in Xenopus oocytes.
        A. Time course of N-type channel (CaV2.2+α2δ1+β1a) activity before and during applications of 10 μM PD 173212 (#P-105) (green) and upon wash. Holding potential was -100 mV and currents were elicited every 10 seconds by 100 ms ramp to +60 mV. B. Superimposed example current traces (plotted against the corresponding ramp voltage) before and during application of 10 μM PD 173212 in green (taken from the experiment described in A).
    References - Scientific background
    • 1. Ryder, T.R. et al. (1999) Bioorg. Med. Chem. Lett. 9, 1813.
    • 2. Hu, L.Y. et al. (1999) Bioorg. Med. Chem. Lett. 9, 2151.
      • Native voltage-gated Ca2+ channels (VGCC, CaV) are pharmacologically classified into at least five different subclasses (L-, N-, P-, Q-, and R-type), the characteristics of which are determined by the pore-forming α1 subunit. The subunit CaV2.2 (α1B) forms N-type Ca2+ channels, which are located primarily on presynaptic nerve terminals of central and peripheral neurons1.

        PD 173212 is a dipeptidyl-amine that acts as a N-type CaV channels blocker. It is the most active small molecule for N-type calcium channel blockade as it inhibits this channel with an IC50 of 36 nM in IMR-32 cells, as measured by using fluorescent technique2. PD 173212 blocks also other CaV channels but to a lesser extent and only at higher concentrations2. In vivo, it prevents tonic seizures in the audiogenic seizure model.

    Target N-type Ca2+ channels
    Last update: 31/12/2018

    PD 173212 (#P-105) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use