GsMTx4 TFA 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 TFA 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 TFA 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 TFA is a spider venom peptide that selectively inhibits cationic-permeablemechanosensitive channels (MSCs)belonging to thePiezoandTRPchannel families. GsMTx4 TFA also blocks cation-selectivestretch-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[1][2][4]. |
| IC50& Target | |
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[1].
GsMTx4 TFA (5 μM) blocks cation-selective stretch-activated channels in astrocytes, cardiac cells, and smooth and skeletal muscle cells[2].
GsMTx4 TFA (2.5 μM, 16 h) significantly diminishes both the leptin-induced AMPK and MLC-2 phosphorylation in breast epithelial cells (MCF10A)[3].
GsMTx4 TFA (500 nM, 48 h) attenuates demyelination induced by the cytotoxic lipid and psychosine (organotypic cerebellar slices)[4].
GsMTx4 TFA (5 μM, 12 h) suppresses neurogenesis and increases astrogenesis in human neural stem cells[5]
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 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[4].
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[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 | 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) |
| 溶解性数据 | In Vitro: H2O : 100 mg/mL(23.75 mM;Need ultrasonic) DMSO : ≥ 50 mg/mL(11.88 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 0.2375 mL | 1.1877 mL | 2.3754 mL | | 5 mM | 0.0475 mL | 0.2375 mL | 0.4751 mL | | 10 mM | 0.0238 mL | 0.1188 mL | 0.2375 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 (sealed storage, away from moisture and light)。-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： PBS Solubility: 50 mg/mL (11.88 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (0.59 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (0.59 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 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。 3. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (0.59 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (0.59 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 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。 4. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (0.59 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (0.59 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 25.0 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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