1. Membrane Transporter/Ion Channel Neuronal Signaling PI3K/Akt/mTOR
  2. Piezo Channel Calcium Channel mTOR PI3K Akt
  3. D-GsMTx4 TFA

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.

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D-GsMTx4 TFA Chemical Structure

D-GsMTx4 TFA Chemical Structure

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Based on 1 publication(s) in Google Scholar

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Description

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[1][2][3][4].

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.

In Vivo

D-GsMTx4 (10 μg/10 μL; s.c.; 1 h after IL-1β injection) TFA significantly inhibits mechanical allodynia and thermal hyperalgesia in the IL-1β-induced orofacial inflammatory pain rat model[4].
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.

Animal Model: Male Sprague Dawley rats with IL-1β-induced inflammatory pain[4]
Dosage: 10 μg/10 μL (normal saline)
Administration: Subcutaneous injection, 1 h after IL-1β injection
Result: Significantly blocked IL-1β-induced mechanical allodynia and thermal hyperalgesia, with antiallodynic effects lasting 3-7 h.
Molecular Weight

4095.84 (free base)

Formula

C185H273N49O45S6.xC2HF3O2

Appearance

Solid

Color

White to off-white

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)

Sequence Shortening

d-(GCLEFWWKCNPNDDKCCRPKLKCSKLFKLCNFSF)-NH2 (Disulfide bridge:Cys2-Cys17, Cys9-Cys23, Cys16-Cys30)

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
In Vitro: 

DMSO : 100 mg/mL (Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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V2

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.

  • Protocol 1

    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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Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.89%

References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
D-GsMTx4 TFA
Cat. No.:
HY-P1410C
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