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CAS No. : 1209500-46-8
MCE 国际站:GsMTx4
产品活性:GsMTx4 是一种蜘蛛毒液肽,选择性地抑制属于 Piezo 和 TRP 通道家族的阳离子可渗透的机械敏感性通道 (MSCs)。GsMTx4 还可阻断阳离子选择性的拉伸激活通道 (SAC),减弱溶血磷脂酰胆碱 (LPC) 诱导的星形胶质细胞毒性和小胶质细胞反应性。GsMTx4 是一种重要的药理学工具,可用于鉴定兴奋性 MSCs 在正常生理学和病理学中的作用。
研究领域:Membrane Transporter/Ion Channel | Neuronal Signaling
作用靶点:TRP Channel | Piezo Channel
In Vitro: 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).
In Vivo: 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.
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