GsMTx4

CAS No. 1209500-46-8

GsMTx4( —— )

Catalog No. M30369 CAS No. 1209500-46-8

GsMTx-4, mechanosensitive and stretch-activated ion channel inhibitor.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    GsMTx4
  • Note
    Research use only, not for human use.
  • Brief Description
    GsMTx-4, mechanosensitive and stretch-activated ion channel inhibitor.
  • Description
    GsMTx-4, mechanosensitive and stretch-activated ion channel inhibitor.
  • In Vitro
    GsMTx4 (5 μM) reduces Piezo1-mediated charge transfer to 38% of its initial levels in HEK293 cells transfected with Piezo1 cDNA.GsMTx4 (5 μM) blocks cation-selective stretch-activated channels in astrocytes, cardiac cells, and smooth and skeletal muscle cells.GsMTx4 (2.5 μM, 16 h) significantly diminishes both the leptin-induced AMPK and MLC-2 phosphorylation in breast epithelial cells (MCF10A).GsMTx4 (500 nM, 48 h) attenuates demyelination induced by the cytotoxic lipid and psychosine (organotypic cerebellar slices). Western Blot Analysis Cell Line:MCF10A cells Concentration:2.5 μM Incubation Time:16 h Result:Diminished both the leptin-induced AMPK and MLC-2 phosphorylation.
  • In Vivo
    GsMTx4 (stereotactic injection, 3 μM of 1 μL, a single dose) is neuroprotective and inhibits lysophosphatidylcholine-induced astrocyte toxicity and demyelination in the cerebral cortex.GsMTx-4 (intraperitoneal injection, 270 μg/kg for a single dose) reduces mechanical allodynia induced by inflammation and by sciatic nerve injury in Von Frey test. Animal Model:Male C57BL/6 mice (toxin-induced focal demyelination of cortical brain tissue)Dosage:3 μM for 1 μL, a single dose.Administration:Stereotactic injection in the left and right cerebral hemispheres (sacrificed 4 days post-injection)Result:Prevented the enhanced increase in microglial reactivity and microglial cell numbers induced by lysophosphatidylcholine (LPC).Prevented LPC-mediated astrocyte toxicity by attenuating the decrease in GFAP+ cells and GFAP fluorescence intensity.Animal Model:Sciatic nerve injury model of male Sprague-Dawley rats Dosage:270 μg/kg, a single dose Administration:Intraperitoneal injection Result:Reduced inflammation-evoked mechanical allodynia.
  • Synonyms
    ——
  • Pathway
    Membrane Transporter/Ion Channel
  • Target
    TRP/TRPV Channel
  • Recptor
    MSCs
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1209500-46-8
  • Formula Weight
    4101.89
  • Molecular Formula
    C185H279N49O45S6
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?H2O : 50 mg/mL (12.21 mM)
  • SMILES
    ——
  • Chemical Name
    Sequence:Gly-Cys-Leu-Glu-Phe-Trp-Trp-Lys-Cys-Asn-Pro-Asn-Asp-Asp-Lys-Cys-Cys-Arg-Pro-Lys-Leu-Lys-Cys-Ser-Lys-Leu-Phe-Lys-Leu-Cys-Asn-Phe-Ser-Phe

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

Gnanasambandam R, et al. GsMTx4: Mechanism of Inhibiting Mechanosensitive Ion Channels. Biophys J. 2017 Jan 10;112(1):31-45.
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