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。
生物活性 | GsMTx4 is a spider venom peptide that selectively inhibits cationic-permeablemechanosensitive channels (MSCs)belonging to thePiezoandTRPchannel families. GsMTx4 also blocks cation-selectivestretch-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 | |
体外研究 (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].
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. |
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体内研究 (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].
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. |
Animal Model: | Sciatic nerve injury model of male Sprague-Dawley rats[6] | Dosage: | 270 μg/kg, a single dose | Administration: | Intraperitoneal injection | Result: | Reduced inflammation-evoked mechanical allodynia. |
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分子量 | |
性状 | |
Formula | |
Sequence Shortening | GCLEFWWKCNPNDDKCCRPKLKCSKLFKLCNFSF-NH2 (Disulfide bridge:Cys2-Cys17, Cys9-Cys17, Cys16-Cys30) |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -80°C | 2 years | | -20°C | 1 year | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: H2O : 50 mg/mL(12.21 mM;Need ultrasonic) DMSO : 50 mg/mL(12.21 mM;Need ultrasonic) 配制储备液 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 |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 1.25 mg/mL (0.31 mM); Clear solution
此方案可获得 ≥ 1.25 mg/mL (0.31 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 1.25 mg/mL (0.31 mM); Clear solution
此方案可获得 ≥ 1.25 mg/mL (0.31 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 1.25 mg/mL (0.31 mM); Clear solution
此方案可获得 ≥ 1.25 mg/mL (0.31 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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