Product Introduction
GsMTx4 TFA is a spider venom-derived peptide isolated from the tarantula Grammostola spatulata (Chilean rose tarantula) that selectively inhibits cation-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. As the most extensively characterized peptide inhibitor of mechanosensitive ion channels, GsMTx4 acts by penetrating the lipid bilayer at the lipid-channel interface and modulating membrane tension-dependent channel gating, thereby reducing channel activation by mechanical stimuli without blocking the pore directly. GsMTx4 also blocks cation-selective stretch-activated channels (SACs) and has been demonstrated to attenuate lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. This peptide serves as an essential pharmacological tool for identifying the roles of excitatory mechanosensitive channels in normal physiology and pathological conditions including cardiac mechanotransduction, muscle function, pain sensation, and neuroinflammation.
Product Features
1. Selective MSC Inhibitor: Potently and selectively inhibits mechanosensitive cation channels of the Piezo and TRP families, serving as the gold-standard pharmacological probe for mechanotransduction research.
2. Gating Modifier Mechanism: Acts at the lipid-channel interface to modulate membrane tension-dependent gating without pore occlusion, preserving channel structural integrity for complementary studies.
3. Neuroprotective Activity: Attenuates LPC-induced astrocyte toxicity and microglial reactivity, demonstrating potential in neuroinflammation and demyelination models.
4. Broad Research Utility: Validated in cardiac mechanotransduction, muscle physiology, pain signaling, and neuronal excitability studies across multiple in vitro and ex vivo systems.
5. High Purity Peptide: Supplied as a synthetic peptide with ¡Ý99% purity for reproducible and reliable pharmacological studies.
Specifications
Size: Available in 1 mg and 5 mg
Molecular Weight: 4115.8 (peptide), 4229.9 (TFA salt)
Sequence: Gly-Cys-Leu-Glu-Phe-Trp-Trp-Lys-Cys-Asn-Pro-Asn-Asp-Asp-Lys-Gln-Cys-Arg-Pro-Lys-Leu-Lys-Cys-Ser-Lys-Leu-Phe-Lys-Leu-Cys-Asn-Phe-Ser-Phe-NH2 (Disulfide bridges: Cys2-Cys17, Cys9-Cys23)
Purity: ¡Ý99%
Solubility: Water: ¡Ý1 mg/mL; saline and buffered solutions: soluble
Storage and Stability
Storage Conditions: Store at -20¡ãC or -80¡ãC, protected from light and moisture. Lyophilized powder is stable under recommended storage conditions.
Shelf Life: The product is stable for 12 months from the date of manufacture when stored as directed. For reconstituted solutions, aliquot into single-use volumes and store at -80¡ãC. Avoid repeated freeze-thaw cycles.
Protocol (For Reference Only)
Important: GsMTx4 is a peptide; handle gently to avoid foaming or shearing. Prepare stock solutions freshly and aliquot to avoid repeated freeze-thaw cycles.
1. Stock Solution Preparation: Reconstitute GsMTx4 TFA in sterile deionized water or saline to prepare a concentrated stock solution (e.g., 100-500 µM). Gently swirl or pipette to dissolve; do not vortex vigorously. Centrifuge briefly to collect contents at the bottom of the vial.
2. In Vitro Working Solution Preparation: Dilute stock solution into extracellular recording buffer or culture medium to achieve working concentrations typically ranging from 0.1-10 µM depending on experimental preparation and channel expression levels.
3. Mechanosensitive Channel Inhibition in Electrophysiology: For patch clamp recordings, perfuse GsMTx4 at 1-5 µM in the extracellular bath solution for 2-5 minutes before and during mechanical stimulation. Monitor channel inhibition as a reduction in mechanically activated current amplitude.
4. Cell Culture Treatment: For astrocyte or microglial studies, pretreat cells with GsMTx4 at 1-10 µM for 30-60 minutes prior to LPC or other stress-inducing stimuli. Assess cellular toxicity by LDH release assay, and microglial reactivity by morphological analysis and inflammatory marker expression.
5. Ex Vivo and Tissue Studies: For organ bath or tissue preparations, include GsMTx4 at 1-5 µM in the perfusate or bathing solution with adequate equilibration time to allow peptide penetration into the tissue.
Precautions
1. GsMTx4 is a peptide and may adsorb to plastic surfaces; use silanized or low-protein-binding tubes and pipette tips for handling dilute solutions.
2. Avoid vigorous vortexing or repeated pipetting of peptide solutions as mechanical stress can denature the peptide and reduce activity.
3. GsMTx4 inhibits MSCs by modifying membrane tension sensing; ensure that the experimental system maintains physiological membrane properties and temperature.
4. The effective concentration of GsMTx4 may vary with cell type, channel subtype, and stimulus modality; perform dose-response experiments to establish optimal inhibitory concentrations for each preparation.
5. For research use only. Not for use in diagnostic or therapeutic procedures.
FAQ (Simplified)
Q1: What is the recommended starting concentration for Piezo channel inhibition?
A1: GsMTx4 at 1-5 µM effectively inhibits Piezo1 and Piezo2 channels in most electrophysiological and cellular assays. For complete inhibition, 5-10 µM may be required depending on expression levels and mechanical stimulus intensity.
Q2: How does GsMTx4 differ from pore-blocking ion channel inhibitors?
A2: GsMTx4 acts as a gating modifier by partitioning into the lipid bilayer and altering membrane tension-dependent channel gating, rather than physically occluding the channel pore. This mechanism preserves the channel in a closed state without interfering with agonist binding sites, making it valuable for studying channel gating mechanisms.
Q3: Can GsMTx4 be used in in vivo studies?
A3: GsMTx4 has been administered in rodent models via local injection (e.g., intramuscular, intrathecal, or intraplantar routes) at doses typically ranging from 10-100 µg per site. Systemic administration has limited utility due to peptide stability and biodistribution. Consult specialized literature for application-specific protocols.
Q4: How should I store reconstituted GsMTx4 solutions?
A4: Aliquot reconstituted stock solutions into single-use volumes, freeze in liquid nitrogen, and store at -80¡ãC. Avoid repeated freeze-thaw cycles. Under these conditions, reconstituted GsMTx4 retains activity for up to 6 months. Working dilutions should be prepared fresh daily.
Disclaimer
1. For Research Use Only. Not for use in diagnostic or therapeutic procedures.
2. Due to the variable nature of biological research, optimization of conditions using a small-scale pilot experiment is strongly recommended before processing valuable samples.
3. This warranty is limited to the replacement of the product. The manufacturer assumes no liability for incidental or consequential damages, including loss of samples or data.
4. Wear appropriate protective clothing and gloves when handling this product.
Ordering Information
Catalog Number: IC-0310692
Product Name: GsMTx4 TFA
Size: 1 mg / 5 mg
Price: 
1 mg: CNY ¥4500.00 / USD $450.00 / EUR €540.00 / JPY ¥81000.00
5 mg: CNY ¥8400.00 / USD $840.00 / EUR €1008.00 / JPY ¥151200.00
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