| Size | Price | Stock | Qty |
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| 500 μg |
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| 1mg |
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| 2mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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Purity: ≥98%
GsMTx4, a TRPC1 and TRPC6 blocker, is a naturally occuring spider venom peptide composed of 34 amino acids, isolated from the Grammostola rosea (Chilean rose) tarantula venom and belongs to the huwentoxin-1 family. It selectively inhibits cation-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology. GsMTx4 significantly attenuates bladder hyperactivity. Also blocks stretch-activated cation channels in astrocytes, cardiac cells, and smooth and skeletal muscle cells. Also inhibits TACAN, a mechanosensitive ion channel involved in the pain response.
| ln Vitro |
GsMTx4 (5 μM) decreased Piezo1-mediated charge transfer to 38% of the starting level in HEK293 cells transfected with Piezo1 cDNA [1]. GsMTx4 (5 μM) inhibits smooth and skeletal muscle cells, cardiomyocytes, and astrocytes' cation-selective stretch-activated channels [2]. In mammary epithelial cells (MCF10A), leptin-induced AMPK and MLC-2 phosphorylation is dramatically reduced by GsMTx4 (2.5 μM, 16 hours) [3]. In organotypic cerebellar slices, GsMTx4 (500 nM, 48 h) attenuates demyelination caused by psychopyrimidine and cytotoxic lipids [4].
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| ln Vivo |
Stereotaxic injection (3 μM, 1 μL, single dose) reduces cerebral cortical demyelination and lysophosphatidylcholine-induced astrocyte toxicity while also having neuroprotective effects [4]. In the Von Frey test, GsMTx-4 (intraperitoneal injection, single dose 270 μg/kg) lessens mechanical allodynia brought on by inflammation and sciatic nerve damage [6].
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| Cell Assay |
Western Blot Analysis[3]
Cell Types: MCF10A Cell Tested Concentrations: 2.5 μM Incubation Duration: 16 hrs (hours) Experimental Results: Leptin-induced phosphorylation of AMPK and MLC-2 was attenuated. |
| Animal Protocol |
Animal/Disease Models: Male C57BL/6 mice (toxin induces focal demyelination in cortical brain tissue) [4]
Doses: 3 μM/1 μL, single dose. Route of Administration: Stereotactic injection in the left and right cerebral hemispheres (sacrifice 4 days after injection) Experimental Results: Prevented lysophosphatidylcholine (LPC)-induced enhanced increase in microglial reactivity and microglia number. Prevents LPC-mediated astrocyte toxicity by attenuating GFAP+ cells and reducing GFAP fluorescence intensity. Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat sciatic nerve injury model [6] Doses: 270 μg/kg, single dose Route of Administration: intraperitoneal (ip) injection Experimental Results: Reduce inflammation-induced mechanical allodynia. |
| 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. |
| Molecular Formula |
C187H280N49F3O47S6
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|---|---|
| Molecular Weight |
4215.91
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| CAS # |
1209500-46-8
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| Related CAS # |
GsMTx4 TFA;D-GsMTx4 TFA;D-GsMTx4
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| SMILES |
S1CC2C(NC(CCCNC(=N)N)C(N3CCCC3C(NC(C(NC(C(NC(C(NC3C(NC(C(NC(C(NC(C(NC(CC4C=CC=CC=4)C(NC(CCCCN)C(NC(CC(C)C)C(NC(C(NC(C(NC(C(NC(C(NC(C(N)=O)CC4C=CC=CC=4)=O)CO)=O)CC4C=CC=CC=4)=O)CC(N)=O)=O)CSSCC(C(N2)=O)NC(C(CCCCN)NC(C(CC(=O)O)NC(C(CC(=O)O)NC(C(CC(N)=O)NC(C2CCCN2C(C(CC(N)=O)NC(C(CSSC3)NC(C(CCCCN)NC(C(CC2=CNC3C=CC=CC2=3)NC(C(CC2=CNC3C=CC=CC2=3)NC(C(CC2C=CC=CC=2)NC(C(CCC(=O)O)NC(C(CC(C)C)NC(C(CS1)NC(CN)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)CC(C)C)=O)CCCCN)=O)CO)=O)=O)CCCCN)=O)CC(C)C)=O)CCCCN)=O)=O)=O
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| Synonyms |
GsMTX 4; GsMTX-4
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~50 mg/mL (~12.21 mM)
DMSO : ~50 mg/mL (~12.21 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (0.31 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (0.31 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.25 mg/mL (0.31 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.2372 mL | 1.1860 mL | 2.3720 mL | |
| 5 mM | 0.0474 mL | 0.2372 mL | 0.4744 mL | |
| 10 mM | 0.0237 mL | 0.1186 mL | 0.2372 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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