產地	國產	規(guī)格	500ug
級別	化工級	證書	ISO系列證書

GsMTx4

GsMTx4 是一種蜘蛛毒液肽，選擇性地抑制屬于 Piezo 和 TRP 通道家族的陽離子可滲透的機械敏感性通道 (MSCs)。GsMTx4 還可阻斷陽離子選擇性的拉伸激huo通道 (SAC)，減弱溶血磷脂酰膽jian (LPC) 誘導的星形膠質細胞毒性和小膠質細胞反應性。GsMTx4 是一種重要的藥理學工具，可用于鑒定興奮性 MSCs 在正常生理學和病理學中的作用。

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^[1]^[2]^[4].

IC₅₀ & Target：MSCs^[1]

體外研究(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[3]

Cell Line:	MCF10A cells
Concentration:	2.5 μM
Incubation Time:	16 h
Result:	Diminished both the leptin-induced AMPK and MLC-2 phosphorylation.

體內研究(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male C57BL/6 mice (toxin-induced focal demyelination of cortical brain tissue)^[4]
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.

分子量：4095.83

性狀：Solid

Formula：C₁₈₅H₂₇₃N₄₉O₄₅S₆

Sequence Shortening

GCLEFWWKCNPNDDKCCRPKLKCSKLFKLCNFSF-NH2 (Disulfide bridge:Cys2-Cys17, Cys9-Cys17, Cys16-Cys30)

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

Sealed storage, away from moisture and light

Powder	-80°C	2 years
	-20°C	1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性數(shù)據(jù)

In Vitro:

H₂O : 50 mg/mL (12.21 mM; Need ultrasonic)

DMSO : 50 mg/mL (12.21 mM; Need ultrasonic)

配制儲備液

濃度溶劑體積質量	1 mg	5 mg	10 mg

1 mM	0.2442 mL	1.2208 mL	2.4415 mL
5 mM	0.0488 mL	0.2442 mL	0.4883 mL
10 mM	0.0244 mL	0.1221 mL	0.2442 mL

請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 儲存時，請在 6 個月內使用，-20°C 儲存時，請在 1 個月內使用。

In Vivo:

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：

——為保證實驗結果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

1.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 1.25 mg/mL (0.31 mM); Clear solution
2.

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1.25 mg/mL (0.31 mM); Clear solution
3.

請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 1.25 mg/mL (0.31 mM); Clear solution

參考文獻

[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.  [Content Brief]
[3]. Anna Acheva, et al. Adipokine Leptin Co-operates With Mechanosensitive Ca 2 +-Channels and Triggers Actomyosin-Mediated Motility of Breast Epithelial Cells. Front Cell Dev Biol. 2021 Jan 6;8:607038.  [Content Brief]
[4]. María Velasco-Estevez, et al. Inhibition of Piezo1 attenuates demyelination in the central nervous system. Glia. 2020 Feb;68(2):356-375.  [Content Brief]
[5]. Medha M Pathak, et al. Stretch-activated ion channel Piezo1 directs lineage choice in human neural stem cells. Proc Natl Acad Sci U S A. 2014 Nov 11;111(45):16148-53.  [Content Brief]
[6]. Seung Pyo Park, et al. A tarantula spider toxin, GsMTx4, reduces mechanical and neuropathic pain. Pain. 2008 Jul;137(1):208-217.  [Content Brief]
注：產品僅用于科研