Certificate of Analysis

VU0529331

Name: VU0529331
Brand: Alomone Labs
SKU: V-155

(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

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

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 K_ir3 family, is part of the larger inwardly rectifying potassium channel (K_ir) 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 addiction^1,2.

Target K_ir3.2, K_ir3.4 channels

Lyophilized Powder

Image & Title

Alomone Labs VU0529331 activates homomeric non-GIRK1-containing GIRK channels expressed in Xenopus oocytes. Representative currents of GIRK2 (K_ir3.2) channels (left) and GIRK4 (K_ir3.4) 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

For research purposes only, not for human use

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