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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GsMTx4 TFA Chemical Structure

GsMTx4 TFA Chemical Structure

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Based on 28 publication(s) in Google Scholar

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GsMTx4 TFA Related Antibodies

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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 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: 

H2O : 100 mg/mL (Need ultrasonic)

DMSO : ≥ 50 mg/mL

*"≥" means soluble, but saturation unknown.

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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 (Infinity mM); 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 (Infinity mM); 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 (Infinity mM); 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: 99.38%

COA (247 KB) RP-HPLC (112 KB) MS (222 KB) Elemental Analysis Report (106 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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