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Home › Products › Ion Channels › K+ Channels › Inward Rectifier K+ Channels › Activators

Certificate of Analysis

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

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 yes
  • Bioassay Tested

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  • Source Synthetic
    MW: 384.4
    Purity: >99% (HPLC)
    Effective concentration 5-100 µM.
    Structure
    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
    PubChem CID 52417637
    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
    References-Activity
    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.
    Scientific background

    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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    Image & Title
    Alomone Labs VU0529331 activates homomeric non-GIRK1-containing GIRK channels expressed in Xenopus oocytes. Representative currents of GIRK2 (Kir3.2) channels (left) and GIRK4 (Kir3.4) channels (right), measured in high K+-containing bath solution at a holding potential of -80 mV. Currents were dose-dependently activated by 25-seconds rapid perfusion with 1 µM, 5 µM, 20 µM and 60 µM VU0529331 (#V-155), as indicated (color legend bottom right). Bar charts in insets (bottom left) show the average effects of VU0529331 concentration on each channel type.
    Data was kindly provided by Prof. Nathan Dascal, Department of Physiology and Pharmacology, Sackler School of Medicine, Tel Aviv University, Israel.
    Last update: 05/02/2023

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    For research purposes only, not for human use

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