D-GsMTx4 TFA
Based on 6 publication(s) in Google Scholar
D-GsMTx4 TFA is a spider peptide and the D enantiomer of GsMTx4 (HY-P1410). D-GsMTx4 TFA inhibits the mechanosensitive ion channel Piezo2. D-GsMTx4 TFA inhibits [Ca2+]i elevation. D-GsMTx4 TFA inhibits mTOR and PI3K-Akt signaling pathways. D-GsMTx4 TFA inhibits mechanical allodynia and thermal hyperalgesia. D-GsMTx4 TFA can be used in researches of mechanical stress, chronic pain and idiopathic pulmonary fibrosis.
For research use only. We do not sell to patients.
- Purity : 99.89%
- Formula: C185H273N49O45S6.xC2HF3O2
- Molecular Weight:4095.84 (free base)
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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)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) D-GsMTx4 TFA
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Customer Validation & Images
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Cell Proliferation/Viability Assay
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WB
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WB
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WB
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Cell Proliferation/Viability Assay
All Calcium Channel Isoforms
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Biological Activity
Description
In Vitro
D-GsMTx4 (5-10 µM) TFA dose-dependently and reversibly inhibits Piezo2-mediated mechanosensitive inward currents in QGP-1 cells and human Piezo2-transfected HEK-293 cells[1].
D-GsMTx4 TFA decreases phosphorylation levels of proteins in the mTOR and PI3K-Akt signaling pathways in primary human lung fibroblasts (HLFs)[2].
D-GsMTx4 (5 µM) TFA inhibits mechanical stimulation-evoked [Ca2+]i increases in cultured DRG neurons from CYP-induced cystitis rats[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
D-GsMTx4 (5-10 μg/50 μL; s.c. or intracisternally) TFA significantly reduces mechanical allodynia in the orofacial neuropathic pain rat model induced by inferior alveolar nerve injury[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague Dawley rats with IL-1β-induced inflammatory pain[4]
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Dosage:10 μg/10 μL (normal saline)
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Administration:Subcutaneous injection, 1 h after IL-1β injection
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Result:Significantly blocked IL-1β-induced mechanical allodynia and thermal hyperalgesia, with antiallodynic effects lasting 3-7 h.
Chemical Information
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Appearance Solid
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Molecular Weight 4095.84 (free base)
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Formula C185H273N49O45S6.xC2HF3O2
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Color White to off-white
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Sequence
d-(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:Cys2-Cys17, Cys9-Cys23, Cys16-Cys30)
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Sequence Shortening
d-(GCLEFWWKCNPNDDKCCRPKLKCSKLFKLCNFSF)-NH2 (Disulfide bridge:Cys2-Cys17, Cys9-Cys23, Cys16-Cys30)
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Shipping
Room temperature in continental US; may vary elsewhere.
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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)
Publications (6)
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Journal Impact Factor
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Most Recent
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EMBO Mol Med
2025 Oct;17(10):2809-2826. PMID: 40921878 -
Curr Biol
Swimming motions evoke Piezo1-dependent Ca2+ events in vascular endothelial cells of larval zebrafish. [Abstract]2025 Dec 15;35(24):6137-6146.e5. PMID: 41237769 -
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Am J Physiol Lung Cell Mol Physiol
Mechanical stretch promotes sustained proliferation and inflammation in developing human airway smooth muscle. [Abstract]2025 Aug 1;329(2):L296-L306. PMID: 40668642
D-GsMTx4 TFA purchased from MedChemExpress. Usage Cited in: Am J Physiol Lung Cell Mol Physiol. 2025 Aug 1;329(2):L296-L306. [Abstract]
D-GsMTx4 (1 μM). The short-term effect of stretch in fASM cell proliferation. fASM cells on Flexcell plates were pretreated with piezo inhibitors for 1h and then were exposed to 5% static stretch with 5% oscillatory stretch (5% CPAP) with continuous presence of the inhibitors. Control cells were exposed to 5% oscillatory stretch only. Cells were harvested after 24h treatment and counted.
D-GsMTx4 TFA purchased from MedChemExpress. Usage Cited in: Am J Physiol Lung Cell Mol Physiol. 2025 Aug 1;329(2):L296-L306. [Abstract]
D-GsMTx4 (1 μM). The protein expressions of Ki67 in fASM cells were determined by JESS.
D-GsMTx4 TFA purchased from MedChemExpress. Usage Cited in: Am J Physiol Lung Cell Mol Physiol. 2025 Aug 1;329(2):L296-L306. [Abstract]
D-GsMTx4 (1 μM). The protein expressions of PCNA in fASM cells were determined by JESS.
D-GsMTx4 TFA purchased from MedChemExpress. Usage Cited in: Am J Physiol Lung Cell Mol Physiol. 2025 Aug 1;329(2):L296-L306. [Abstract]
D-GsMTx4 (1 μM). The protein expressions of Cyclin E1 in fASM cells were determined by JESS.
D-GsMTx4 TFA purchased from MedChemExpress. Usage Cited in: Am J Physiol Lung Cell Mol Physiol. 2025 Aug 1;329(2):L296-L306. [Abstract]
The long-term effect of stretch in fASM cell proliferation. fASM cells on Flexcell plates were pretreated with D-GsMTx4 (1 μM) for 1h and then were exposed to 5% static stretch with 5% oscillatory stretch (5% CPAP) with or without the inhibitors. Control cells were exposed to 5% oscillatory stretch only. Cells were harvested after 24h treatment and seeded into 96-well plates. After 3-day culture without stretch, cell proliferation was measured by CyQUANT assay.
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Pediatr Res
Stretch, Piezo channels, and store operated calcium entry in developing human airway smooth muscle. [Abstract]2026 Apr 24. PMID: 42032191
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL; Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
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Fibrosis/Collagen Morphometry
Fibrosis and collagen morphometry is based on the quantitative visualization of fibrillar collagen deposition in tissue sections using histochemical stains such as Sirius Red (Picrosirius Red) or Masson's trichrome, followed by image-based or polarization-enhanced analysis to estimate collagen proportional area as a surrogate of extracellular matrix accumulation during fibrotic remodeling. Sirius Red combined with polarized light microscopy enhances detection of collagen fibers due to birefringence properties, enabling more specific visualization of collagen type I and III fibrils compared to conventional bright-field histology, while whole-section or region-restricted digital morphometry reduces field-selection bias in fibrosis assessment. Alternative quantitative approaches include second harmonic generation (SHG) and two-photon excited fluorescence microscopy, which enable label-free detection of fibrillar collagen and have been validated against histological staining and biochemica
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Collagen: Sirius Red Staining
Sirius Red or picrosirius red staining is a histochemical method for visualizing collagen-rich extracellular matrix in tissue sections, and collagen fibers are detected as red-stained structures under bright-field microscopy with enhanced birefringence under polarized light. Picrosirius red is useful for assessing total collagen organization, distribution, and fibrosis burden, but polarized color should not be interpreted as a definitive collagen type I versus type III readout because color is affected by fiber orientation, thickness, and packing.
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Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
Masson’s Trichrome (collagen/trichrome staining) is a histological technique that differentially stains tissue compartments using sequential acidic dyes to distinguish collagen from muscle and cytoplasmic components based on dye affinity and tissue permeability differences, enabling visualization of fibrosis and connective tissue architecture in histological sections. The classical formulation typically uses Weigert's iron hematoxylin for nuclear staining, Biebrich scarlet-acid fuchsin for cytoplasm and muscle, and aniline blue (or light green variants) for collagen, producing a characteristic blue/green collagen signal contrasted against red cytoplasm and dark nuclei. The staining principle relies on selective displacement of smaller dye molecules by larger anionic dyes in collagen-rich regions under controlled acidified conditions, which enhances collagen-specific dye retention. This property makes the method widely used for fibrosis assessment in organs such as heart, liver, lung, a
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Two-electrode voltage clamp in Xenopus oocytes
Two-electrode voltage clamp measures whole-oocyte membrane current from Xenopus oocytes expressing exogenous ion channels, receptors, or transporters; one intracellular microelectrode senses membrane voltage, and the second injects current so the amplifier can hold the membrane at command voltages while recording the compensating current as the functional readout. The method is suited to Xenopus oocytes because their large size supports microinjection and intracellular electrode impalement, but the large membrane area can limit voltage-clamp speed and accuracy, especially for large or fast currents.
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
Purity & Documentation
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Data Sheet (298 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Alcaino C, et al. Mechanosensitive ion channel Piezo2 is inhibited by D-GsMTx4. Channels (Austin). 2017 May 4;11(3):245-253. doi: 10.1080/19336950.2017.1279370. Epub 2017 Jan 13. Erratum for: Addendum to: Wang F, Knutson K, Alcaino C, Linden DR, Gibbons SJ, Kashyap PK, Grover M, Oeckler R, Gottlieb PA, Li HJ, et al. Mechanosensitive ion channel Piezo2 is important for enterochromaffin cell response to mechanical forces. J Physiol. 2017; 595(1):79-91. [Content Brief]
[3]. Liu L, et al. Piezo2 Channel Upregulation is Involved in Mechanical Allodynia in CYP-Induced Cystitis Rats. Mol Neurobiol. 2023 Sep;60(9):5000-5012. [Content Brief]
[4]. Jo MJ, et al. Blockade of Piezo2 Pathway Attenuates Inflammatory and Neuropathic Pain in the Orofacial Area. Pain Res Manag. 2024 Sep 27;2024:9179928. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
D-GsMTx4 TFA Related Classifications
HY-P1410C Related Classifications
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