产品
编 号:F071860
分子式:C185H273N49O45S6
分子量:4095.84
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500μg
2160
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1mg
4000
In-stock
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生物活性:
GsMTx4 is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology.

体内研究:
GsMTx4 (stereotactic injection, 3 μM of 1 μL, a single dose) is neuroprotective and inhibits lysophosphatidylcholine-induced astrocyte toxicity and demyelination in the cerebral cortex.GsMTx-4 (intraperitoneal injection, 270 μg/kg for a single dose) reduces mechanical allodynia induced by inflammation and by sciatic nerve injury in Von Frey test.Animal Model:Male C57BL/6 mice (toxin-induced focal demyelination of cortical brain tissue)
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
Dosage:270 μg/kg, a single dose
Administration:Intraperitoneal injection
Result:Reduced inflammation-evoked mechanical allodynia.

体外研究:
GsMTx4 (5 μM) reduces Piezo1-mediated charge transfer to 38% of its initial levels in HEK293 cells transfected with Piezo1 cDNA.GsMTx4 (5 μM) blocks cation-selective stretch-activated channels in astrocytes, cardiac cells, and smooth and skeletal muscle cells.GsMTx4 (2.5 μM, 16 h) significantly diminishes both the leptin-induced AMPK and MLC-2 phosphorylation in breast epithelial cells (MCF10A).GsMTx4 (500 nM, 48 h) attenuates demyelination induced by the cytotoxic lipid and psychosine (organotypic cerebellar slices).
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