2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel Piezo Channel
  4. GsMTx4 TFA

GsMTx4 TFA is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 TFA also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 TFA is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology.

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Based on 112 publication(s) in Google Scholar

Other Forms of GsMTx4 TFA:

GsMTx4 TFA Related Antibodies

Top Publications Citing Use of Products

112 Publications Citing Use of MCE GsMTx4 TFA

Flow Cytometry
Cell Proliferation/Viability Assay
In Vivo Efficacy Study
WB
Cell Migration/Invasion Assay

    GsMTx4 TFA purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 Aug 21;10(1):269.  [Abstract]

    Flow cytometry analysis showing that Yoda1-induced Ca²⁺ influx is blocked by GsMTx4（0-1 μM; 120 s）.

    GsMTx4 TFA purchased from MedChemExpress. Usage Cited in: Nat Biotechnol. 2025 Nov 10.  [Abstract]

    Administration of GsMTx4 (5 μM; 5 μL) reduced the blood product clearance of UDC, as assessed by hematoma volumes across treatment groups.

    GsMTx4 TFA purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Mar 8;16(1):2329.  [Abstract]

    Phospho-RAB10 (T73) signal measured by western blot in WT Henle 407 cells. The cells were treated with the PIEZO1 inhibitor GsMTx4 (10 μM; 30 min), LPS and/or the PIEZO1 agonist Yoda1, and cell lysates were collected and immunoblotted for phospho-RAB10 (T73), total RAB10, or ß-actin (loading control) .

    GsMTx4 TFA purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jul 25;16(1):6868.  [Abstract]

    GsMTx4（5 μM; 30 min）- treated BxPC3 DUOX1/2 WT cells, green lines indicate initial wound edges at t = 0 h, red lines indicate wound edges at the indicated timepoints, red arrows show area of damaged cells.

    GsMTx4 TFA purchased from MedChemExpress. Usage Cited in: Cell. 2024 Jun 20;187(13):3409-3426.e24.  [Abstract]

    WT CD8⁺ T cells treated with DMSO or a Piezo1 inhibitor (GsMTx4, 5 μM; 2 h).

    View All TRP Channel Isoform Specific Products:

    View All Isoforms
    TRPA1 TRPC3 TRPC4 TRPC5 TRPC6 TRPC7 TRPM8 TRPM2 TRPM3 TRPM4 TRPM7 TRPML1 TRPML2 TRPML3 TRPV1 TRPV2 TRPV3 TRPV4 TRPV6

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    • Purity & Documentation

    • References

    • Customer Review

    Description

    GsMTx4 TFA is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 TFA also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 TFA is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology[1][2][4].

    IC50 & Target

    MSCs[1]
    In Vitro

    GsMTx4 TFA (5 μM) reduces Piezo1-mediated charge transfer to 38% of its initial levels in HEK293 cells transfected with Piezo1 cDNA[1].
    GsMTx4 TFA (5 μM) blocks cation-selective stretch-activated channels in astrocytes, cardiac cells, and smooth and skeletal muscle cells[2].
    GsMTx4 TFA (2.5 μM, 16 h) significantly diminishes both the leptin-induced AMPK and MLC-2 phosphorylation in breast epithelial cells (MCF10A)[3].
    GsMTx4 TFA (500 nM, 48 h) attenuates demyelination induced by the cytotoxic lipid and psychosine (organotypic cerebellar slices)[4].
    GsMTx4 TFA (5 μM, 12 h) suppresses neurogenesis and increases astrogenesis in human neural stem cells[5]

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    GsMTx4 TFA Related Antibodies

    Western Blot Analysis[3]

    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 TFA (stereotactic injection, 3 μM for 1 μL, a single dose) is neuroprotective and inhibits lysophosphatidylcholine-induced astrocyte toxicity and demyelination in the cerebral cortex[4].
    GsMTx-4 TFA (intraperitoneal injection, 270 μg/kg for a single dose) reduces mechanical allodynia induced by inflammation and by sciatic nerve injury in Von Frey test[6].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Male C57BL/6 mice (toxin-induced focal demyelination of cortical brain tissue)[4]
    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[6]
    Dosage: 270 μg/kg, a single dose
    Administration: Intraperitoneal injection
    Result: Reduced inflammation-evoked mechanical allodynia.
    Molecular Weight

    4095.84 (free base)

    Formula

    C185H273N49O45S6.xC2HF3O2
    Appearance

    Solid

    Color

    White to off-white

    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-NH2
    Sequence Shortening

    GCLEFWWKCNPNDDKCCRPKLKCSKLFKLCNFSF-NH2 (Disulfide bridge:Cys2-Cys17, Cys9-Cys17, Cys16-Cys30)
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    Sealed storage, away from moisture and light

    Powder -80°C 2 years
    -20°C 1 year

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL

    H2O : 16.67 mg/mL (Need ultrasonic)

    *"≥" means soluble, but saturation unknown.

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    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL; Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL; Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  PBS

      Solubility: 50 mg/mL; Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.85%

    SDS (252 KB)

    COA (261 KB) RP-HPLC (255 KB) MS (202 KB)

    Handling Instructions (2659 KB)
    References
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    GsMTx4 TFA Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    GsMTx4GsMTx 4GsMTx-4TRP ChannelPiezo ChannelTransient receptor potential channelsMSCsSACsTRPmyelinationPiezo1hypertensionLPCInhibitorinhibitorinhibit

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