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XEN907

A Specific Blocker of NaV1.7 Channels

Cat #: X-105
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 351.1
    Purity: >99% (HPLC)
    Effective concentration 1 nM - 10 µM.
    Structure
    Chemical name 1'-pentylspiro[6H-furo[2,3-f][1,3]benzodioxole-7,3'-indole]-2'-one.
    Molecular formula C21H21N4O.
    CAS No.: 912656-34-9
    PubChem CID 11998198
    Activity XEN907 is a NaV1.7 channel blocker with an IC50 value of 5 nM for the channel in its inactivated state1.
    References-Activity
    1. Chowdhury, S. et al. (2011) Bioorg. Med. Chem. Lett. 21, 3676.
    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 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 XEN907 blocks NaV1.7 channels expressed in Xenopus oocytes. 
      Alomone Labs XEN907 blocks NaV1.7 channels expressed in Xenopus oocytes. 
      A. Time course of NaV1.7 current amplitude and inhibition by 10 µM XEN907 (#X-105). Currents were elicited by application of a 100 ms voltage step to 0 mV (H.P= -70 mV, to induce inactivation), every 10 seconds. B. Superimposed example traces of current responses before and during perfusion of 10 µM XEN907, as indicated.
    References - Scientific background
    1. Chowdhury, S. et al. (2011) Bioorg. Med. Chem. Lett. 21, 3676.
    Scientific background

    Voltage-gated sodium (NaV) channels contribute to physiological and pathophysiological electrical signaling in nerve and muscle cells. NaV1.7 is highly expressed on the axons of somatic afferent neurons and is thought to play an important role in the signaling of inflammatory pain.

    XEN907 is a synthetic blocker of NaV1.7 channels. It has an effective concentration of 1 nM – 10 μM and an IC50 of 5 nM for NaV1.7 in its inactive state. XEN907 is highly specific for NaV1.7 and at a concentration of 10 μM was not found to have significant activity against some 63 receptors and transporters examined1. XEN907 is not toxic and has favorable hepatocyte metabolic stability in humans and dogs, although inhibition of CYP3A4 was observed in a recombinant human enzyme assay. XEN907 has 97% plasma protein binding property in rat. XEN907 exhibits modest bioavailability of 13% and a T0.5 of 2.6±0.1 hours. XEN907 is extensively distributed when administered intravenously and has a clearing rate of 9.4±1.7 (L/h/kg)1.

    Target NaV1.7 channels
    Lyophilized Powder
    Last update: 11/04/2021

    XEN907 (#X-105) is a highly pure, synthetic, and biologically active compound.

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    For research purposes only, not for human use
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