GsMTx4

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^[1][2][4]. IC50 & Target:MSCs^[1] In Vitro: GsMTx4 (5 μM) reduces Piezo1-mediated charge transfer to 38% of its initial levels in HEK293 cells transfected with Piezo1 cDNA^[1].
GsMTx4 (5 μM) blocks cation-selective stretch-activated channels in astrocytes, cardiac cells, and smooth and skeletal muscle cells^[2].
GsMTx4 (2.5 μM, 16 h) significantly diminishes both the leptin-induced AMPK and MLC-2 phosphorylation in breast epithelial cells (MCF10A)^[3].
GsMTx4 (500 nM, 48 h) attenuates demyelination induced by the cytotoxic lipid and psychosine (organotypic cerebellar slices)^[4].
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^[4].
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^[6].