GsMTx4 TFA
PRODUCTS SPECIFICATIONS
DESCRIPTION
Overview
| MDL | - |
|---|---|
| Molecular Weight | 4209.85 |
| Molecular Formula | C187H274N49F3O47S6 |
| SMILES | - |
15 Publications Citing Use of MCE
- [1]Neuron. 2022 Nov 8;S0896-6273(22)00954-0.
- [2]Research (Wash D C). 2023 Jan 20.
- [3]Materials Today Advances. 2023, 17: 100325.
- [4]Hypertension. 2021 Sep;78(3):647-660.
- [5]Cell Discov. 2022 Sep 6;8(1):84.
- [6]Cell Biosci. 2023 Jan 12;13(1):7.
- [7]FASEB J. 2022 Aug;36(8):e22423.
- [8]Am J Physiol Cell Physiol. 2022 Aug 15.
- [9]Am J Physiol Lung Cell Mol Physiol. 2022 May 1;322(5):L737-L760.
- [10]J Neurochem. 2021 Nov 10.
- [11]Stem Cells Int. 29 Jul 2022.
- [12]J Gastroenterol Hepatol. 2021 Jun 24.
- [13]Biochem Biophys Res Commun. 2022.
- [14]bioRxiv. 2023 Jan 13.
- [15]Research Square Print. December 8th, 2022.
Summary
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]
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]
.
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. |
Appearance
Solid
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
H 2 O : 100 mg/mL ( 23.75 mM ; Need ultrasonic)
DMSO : ≥ 50 mg/mL ( 11.88 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 0.2375 mL | 1.1877 mL | 2.3754 mL |
| 5 mM | 0.0475 mL | 0.2375 mL | 0.4751 mL |
| 10 mM | 0.0238 mL | 0.1188 mL | 0.2375 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (11.88 mM); Clear solution; Need ultrasonic
-
2.
-
3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (0.59 mM); Clear solution
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (0.59 mM); Clear solution
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.
- [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.
- [4] María Velasco-Estevez, et al. Inhibition of Piezo1 attenuates demyelination in the central nervous system. Glia. 2020 Feb;68(2):356-375.
- [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.
- [6] Seung Pyo Park, et al. A tarantula spider toxin, GsMTx4, reduces mechanical and neuropathic pain. Pain. 2008 Jul;137(1):208-217.