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GsMTx4 TFA
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
包装与价格:
包装价格(元)
500 μg电议
1mg电议
5mg电议
10mg电议
50mg电议

产品介绍
GsMTx4 TFA 是一种蜘蛛毒液肽,选择性地抑制属于PiezoTRP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

MSCs[1]

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.
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.
分子量

4209.85

性状

Solid

Formula

C187H274N49F3O47S6

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°C2 years
-20°C1 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
浓度溶剂体积质量1 mg5 mg10 mg
1 mM0.2375 mL1.1877 mL2.3754 mL
5 mM0.0475 mL0.2375 mL0.4751 mL
10 mM0.0238 mL0.1188 mL0.2375 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。

    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
  • 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。

    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
  • 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。