GsMTx4|西域试剂

GsMTx4,98.71%

产品编号：Bellancom-P1410| 分子式：C₁₈₅H₂₇₃N₄₉O₄₅S₆| 分子量：4095.83

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货号	价格	库存与货期
Bellancom-P1410	￥2700.00	杭州北京（现货）
Bellancom-P1410	￥5000.00	杭州北京（现货）
Bellancom-P1410	￥18000.00	杭州北京（现货）

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GsMTx4

产品介绍

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-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^[4].

体外研究

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

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

Western Blot Analysis

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

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].

西域 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.

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.

体内研究

西域 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.

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.

体内研究

西域 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.

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.

性状

Solid

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

浓度溶剂体积质量	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

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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
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。