GSMTX-4
GSMTX-4 Basic information
- Product Name:
- GSMTX-4
- 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
- GsMTx-4, mechanosensitive and stretch-activated ion channel inhibitor
- 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(Cys2&Cys17,Cys9&Cys23,Cys16&Cys30 bridge)
- GsMTx4 ，P1205
- CAS:
- 1209500-46-8
- MW:
- 0
- Mol File:
- Mol File
GSMTX-4 Chemical Properties
- 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)
GSMTX-4 Usage And Synthesis
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. |
| 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
-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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