VU0529331

(2-(3,4-dimethylphenyl)-3-(1H-pyrrol-1-yl)pyrrolo[3,4-c]pyrazol-5(2H,4H,6H)-yl)(pyrazin-2-yl)methanone
An Activator of Homomeric and Non-GIRK1-Containing GIRK Channels
  • New
Cat #: V-155
Alternative Name (2-(3,4-dimethylphenyl)-3-(1H-pyrrol-1-yl)pyrrolo[3,4-c]pyrazol-5(2H,4H,6H)-yl)(pyrazin-2-yl)methanone
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 384.4
    Purity: >99% (HPLC)
    Effective concentration 5-100 µM.
    Chemical name [2-(3,4-dimethylphenyl)-3-pyrrol-1-yl-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl]-pyrazin-2-ylmethanone.
    Molecular formula C22H20N6O.
    CAS No.: 1286725-49-2.
    Activity VU0529331 is a novel activator of homomeric and of non-GIRK1-containing G-protein-activated inward rectifier potassium (GIRK) channels. VU0529331 was shown to significantly activate GIRK2 and GIRK4 homomeric channels expressed in HEK293 cells (GIRK2 EC50=5.1 µM).1
      • Kozek, K.A. et al. (2018) ACS Chem. Neurosci. doi: 10.1021/acschemneuro.8b00287.
    Shipping and storage Store at -20°C.
    Solubility Soluble to 15 mM in DMSO with gentle warming. Centrifuge all products before handling (10000 x g 5 min).
    Storage of solutions Store at -20°C for several months. It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.
      • Alomone Labs VU0529331 activates homomeric GIRK2 (Kir3.2) channels expressed in Xenopus oocytes.
        Representative time course of GIRK2 (Kir3.2) current, measured in continuously applied high K+-containing bath solution (top dotted line), and activated by 30 µM VU0529331 (#V-155), as indicated, at a holding potential of -80 mV.
      • Kozek, K.A. et al. (2018) ACS Chem. Neurosci. doi: 10.1021/acschemneuro.8b00287.
      • Tabak, G. et al. (2019) Sci. Rep. 9, 508.
      • VU0529331 is an activator of the homomeric and of non-GIRK1-containing GIRK channels. The activity of the compound is much stronger on non-GIRK1/X channels. VU0529331 does not change the potassium selectivity or rectification of GIRK channels1. VU0529331 activates GIRK2 and GIRK4 homomeric channels expressed in HEK293 cells and demonstrates EC50 values of 5.1 and 22.3 µM respectively1.

        The GIRK family, also known as the Kir3 family, is part of the larger inwardly rectifying potassium channel (Kir) family. GIRK channels play an important role in the regulation of cellular excitability. GIRK channels are heterotetrameric or homotetrameric combinations of the GIRK1−GIRK4 subunits. GIRK channels are associated with a variety of neurological disorders and alcohol and drug addiction1,2.

    Target Kir3.2, Kir3.4 channels

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    Last update: 28/03/2019

    VU0529331 (#V-155) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use