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VU590 dihydrochloride

ML111, AOB1540
A Blocker of Kir1.1 and Kir7.1 K+ Channels
Cat #: V-130
Alternative Name ML111, AOB1540
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 561.46
    Purity: >98% (HPLC)
    Effective concentration 0.1-25 µM.
    Structure
    Chemical name 7,13-bis[(4-nitrophenyl)methyl]-1,4,10-trioxa-7,13-diazacyclopentadecane dihydrochloride.
    Molecular formula C24H34Cl2N4O7.
    CAS No.: 313505-85-0.
    PubChem CID 71433535
    Activity VU590 inhibits ROMK1 channels in a dose-dependent manner with an IC50 of 294 nM. Inhibits Kir7.1 at micromolar concentrations, whilst having no effect on Kir2.1 or Kir4.11.
    References-Activity
    1. Lewis, L.M. et al. (2009) Mol. Pharmacol. 76, 1094.
    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 Up to 100 mM in 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.
    Our bioassay
    • Alomone Labs VU590 dihydrochloride blocks Kir1.1 channels expressed in Xenopus oocytes.
      Alomone Labs VU590 dihydrochloride blocks Kir1.1 channels expressed in Xenopus oocytes.
      A. Time course of Kir1.1 currents at +30 mV. Currents were elicited by 150 ms voltage ramp from -120 mV to +60 mV (HP -90 mV, no leak subtraction). VU590 dihydrochloride (#V-130) applied at 1 µM and 10 µM, as indicated, inhibited Kir1.1 channels current in a dose dependent and partially reversible manner. B. Current traces upon application of control, or of 1 µM and 10 µM VU590 dihydrochloride (as indicated).
    References - Scientific background
    1. Lewis, L.M. et al. (2009) Mol. Pharmacol. 76, 1094.
    Scientific background VU590 dihydrochloride is a synthetic blocker of Kir1.1 channel with an IC50 of 294nM for Kir1.1 channel. VU590 also inhibits Kir7.1 channels at micromolar concentrations whilst having no effect on Kir2.1 or Kir4.1 channels. At a voltage of -120mV VU590 inhibits Kir1.1 currents by 95.3±0.5%. Inhibition of the Kir1.1 channel is dose dependent. 10 µM of VU590 cause a slow rate inhibition of Kir1.1 with a time constant of 40.0±0.5 s suggesting that VU590 first has to cross the plasma membrane in order to reach its binding site. Kir1.1 block by VU590 is relieved by hyperpolarizing pulses and increased extracellular K+ concentrations. This is hypothesized to be achieved by increased blocker dissociation into the cytoplasmic compartment when exposed to these conditions. The binding site of VU590 within the Kir1.1 channel is yet to be determined1.
    Target Kir1.1, Kir7.1 channels
    Last update: 23/08/2020

    VU590 dihydrochloride (#V-130) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
    Shipping and Ordering information