GsMTx4 TFA is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 TFA also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 TFA is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology.
性状
Solid
IC50 & Target[1][2]
MSCs
体外研究(In Vitro)
GsMTx4 TFA (5 μM) reduces Piezo1-mediated charge transfer to 38% of its initial levels in HEK293 cells transfected with Piezo1 cDNA.GsMTx4 TFA (5 μM) blocks cation-selective stretch-activated channels in astrocytes, cardiac cells, and smooth and skeletal muscle cells.GsMTx4 TFA (2.5 μM, 16 h) significantly diminishes both the leptin-induced AMPK and MLC-2 phosphorylation in breast epithelial cells (MCF10A).GsMTx4 TFA (500 nM, 48 h) attenuates demyelination induced by the cytotoxic lipid and psychosine (organotypic cerebellar slices).GsMTx4 TFA (5 μM, 12 h) suppresses neurogenesis and increases astrogenesis in human neural stem cells has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
GsMTx4 TFA (stereotactic injection, 3 μM for 1 μL, a single dose) is neuroprotective and inhibits lysophosphatidylcholine-induced astrocyte toxicity and demyelination in the cerebral cortex.
GsMTx-4 TFA (intraperitoneal injection, 270 μg/kg for a single dose) reduces mechanical allodynia induced by inflammation and by sciatic nerve injury in Von Frey test. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Sealed storage, away from moisture and lightPowder -80°C 2 years;-20°C 1 year
[1]. Gnanasambandam R, et al. GsMTx4: Mechanism of Inhibiting Mechanosensitive Ion Channels. Biophys J. 2017 Jan 10;112(1):31-45. [2]. T M Suchyna, et al. Identification of a peptide toxin from Grammostola spatulata spider venom that blocks cation-selective stretch-activated channels. J Gen Physiol. 2000 May;115(5):583-98. [3]. Anna Acheva, et al. Adipokin
溶解度数据
In Vitro: H2O : 100 mg/mL (23.75 mM; Need ultrasonic)DMSO : ≥ 50 mg/mL (11.88 mM)