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

GsMTx4 TFA 

Cat. No.: HY-P1410A Purity: 99.38%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

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GsMTx4 TFA Chemical Structure

GsMTx4 TFA Chemical Structure

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500 μg USD 270 In-stock
1 mg USD 500 In-stock
5 mg USD 1800 In-stock
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Based on 26 publication(s) in Google Scholar

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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.

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.

In Vivo:
  • 1.

    Add each solvent one by one:  PBS

    Solubility: 50 mg/mL (Infinity mM); Clear solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (Infinity mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (Infinity mM); Clear solution

  • 4.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (Infinity mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.38%

References
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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.

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GsMTx4 TFA
Cat. No.:
HY-P1410A
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