| Identification | Back Directory | [Name]
GSMTX-4 | [CAS]
1209500-46-8 | [Synonyms]
GSMTX-4
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 | [MDL Number]
MFCD03456972 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [form ]
Solid | [color ]
White to off-white | [Water Solubility ]
Water : 16.67 mg/mL | [Sequence]
H-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(Disulfide bridge: 2-17,9-23,16-30) |
| Hazard Information | Back Directory | [Uses]
GsMTx4 is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology[1][2][4]. | [Definition]
ChEBI: GsMTx4 is peptide that acts as a mechanosensitive ion channel blocker. | [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[4].
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[6]. | 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.
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| 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. |
| [storage]
Store at -20°C | [References]
[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. DOI:10.1085/jgp.115.5.583
[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. DOI:10.3389/fcell.2020.607038
[4] María Velasco-Estevez, et al. Inhibition of Piezo1 attenuates demyelination in the central nervous system. Glia. 2020 Feb;68(2):356-375. DOI:10.1002/glia.23722
[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. DOI:10.1073/pnas.1409802111
[6] Seung Pyo Park, et al. A tarantula spider toxin, GsMTx4, reduces mechanical and neuropathic pain. Pain. 2008 Jul;137(1):208-217. DOI:10.1016/j.pain.2008.02.013 |
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