GsMTx4 TFA

• CAT Number: I046117
• Molecular Formula: C185H273N49O45S6.xC2HF3O2
• Molecular Weight: 4095.84 (free base)
• Purity: ≥95%

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].
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]
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].

Reference

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

[2]. T M Suchyna, et al. Identification of a peptide toxin from Grammostola spatulata spider venom that blocks cation-selective stretch-activated channels. J Gen Physiol. 2000 May;115(5):583-98.
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[3]. Anna Acheva, et al. Adipokine Leptin Co-operates With Mechanosensitive Ca 2 +-Channels and Triggers Actomyosin-Mediated Motility of Breast Epithelial Cells. Front Cell Dev Biol. 2021 Jan 6;8:607038.
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[4]. María Velasco-Estevez, et al. Inhibition of Piezo1 attenuates demyelination in the central nervous system. Glia. 2020 Feb;68(2):356-375.
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[5]. Medha M Pathak, et al. Stretch-activated ion channel Piezo1 directs lineage choice in human neural stem cells. Proc Natl Acad Sci U S A. 2014 Nov 11;111(45):16148-53.
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[6]. Seung Pyo Park, et al. A tarantula spider toxin, GsMTx4, reduces mechanical and neuropathic pain. Pain. 2008 Jul;137(1):208-217.
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