GsMTx4
目录号 : GC38465
GsMTx4是一种由34个氨基酸组成的蜘蛛毒素肽，属于huwentoxin-1家族。
Cas No.:1209500-46-8
Sample solution is provided at 25 µL, 10mM.
GsMTx4 is a 34 amino acid spider venom peptide and belongs to the huwentoxin-1 family[1]. GsMTx4 selectively inhibits cation-permeable mechanosensitive channels (MSCs) belonging to the Piezo, TRPC1 and TRPC6 channels.
GsMTx4 is similar to many other channel-active peptides isolated from spider venom, which are small (3–5 kD) amphipathic molecules built on a conserved inhibitory cysteine-knot (ICK) backbone[4].GsMTx4 has high potency for inhibiting mechanosensitive channels, and its inhibition is not stereospecific, i.e., both its enantiomers (L- and D-form) inhibiting MSCs[3].
GsMTx4 significantly attenuates bladder hyperactivity[2]. Intraperitoneal injection of GsMTx-4 has been shown to reduce mechanical hyperalgesia induced by carrageenan or sciatic nerve injury[5], although it does not inhibit SAC currents in cultured DRG neurons[6].
GsMTx4 is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology[4].
References
[1]. Suchyna TM, 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.
[2]. Liu Q, et al. Increased Piezo1 channel activity in interstitial Cajal-like cells induces bladder hyperactivity by functionally interacting with NCX1 in rats with cyclophosphamide-induced cystitis. Exp Mol Med. 2018 May 7;50(5):60.
[3]. Suchyna T.M., Tape S.E., Gottlieb P.A. Bilayer-dependent inhibition of mechanosensitive channels by neuroactive peptide enantiomers. Nature. 2004;430:235–240.
[4]. Gnanasambandam R, et al. GsMTx4: Mechanism of Inhibiting Mechanosensitive Ion Channels. Biophys J. 2017 Jan 10;112(1):31-45.
[5]. Park SP, et al. A tarantula spider toxin, GsMTx4, reduces mechanical and neuropathic pain. Pain. 2008;137:208–217.
[6]. Drew LJ, , et al.. High-threshold mechanosensitive ion channels blocked by a novel conopeptide mediate pressure-evoked pain. PLoS ONE. 2007;2:e515.
GsMTx4是一种由34个氨基酸组成的蜘蛛毒素肽，属于huwentoxin-1家族[1]。GsMTx4选择性地抑制属于Piezo、TRPC1和TRPC6通道的阳离子渗透机械敏感通道（MSCs）。
GsMTx4是从蜘蛛毒液中分离出来的一种类似于许多其他通道活性肽的物质，它们都是建立在保守的抑制性半胱氨酸结（ICK）骨架上的小型（3-5 kD）两亲分子[4]。GsMTx4对于抑制机械敏感通道具有很高的效力，并且其抑制作用不具有立体特异性，即其左旋和右旋异构体均能够抑制MSCs[3]。
GsMTx4可以显著减轻膀胱过度活动[2]。已经证明，通过腹腔注射GsMTx-4可以减少由卡拉胶或坐骨神经损伤引起的机械性高敏感性[5]，但它不会抑制培养的DRG神经元中的SAC电流[6]。
GsMTx4是一种重要的药理学工具，用于确定这些兴奋性MSC在正常生理和病理中的作用[4]。
| Cell experiment [1]: | |
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Cell lines |
HEK 293 cells |
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Preparation method |
For Piezo1 channels, the extracellular solution contained 145 mM NaCl, 5 mM KCl, 3 mM MgCl2, 0.1 mM CaCl2, and 10 mM HEPES (pH 7.4). The pipette solution contained 133 mM CsCl, 10 mM HEPES (pH 7.4). The inhibition produced by application of GsMTx4 was followed by ∼60 s of washout, followed by application of WT GsMTx4 as a control. |
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Reaction Conditions |
5 μM GsMTx4, 40s |
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Applications |
GsMTx4 is a spider venom peptide that inhibits cationic mechanosensitive channels (MSCs). A model placing GsMTx4 at the membrane surface, where it is stabilized by the lysines, and occupying a small fraction of the surface area in unstressed membranes. When applied tension reduces lateral pressure in the lipids, the peptides penetrate deeper acting as “area reservoirs” leading to partial relaxation of the outer monolayer, thereby reducing the effective magnitude of stimulus acting on the MSC gate. |
| Animal experiment [2]: | |
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Animal models |
Male C57BL/6 mice |
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Dosage form |
To the WT and ClockΔ19/Δ19 mice, GsMTx4 or vehicle was administered via intraperitoneal injection (IP) at two different time-points, Z12- and ZT0-IP (higher and lower Piezo1 expression periods in the WT mice, respectively). The WT and ClockΔ19/Δ19 mice were injected with 0.75 (low dose-IP) or 1.5 mg/kg (high dose-IP) of GsMTx4 in 100 μL of distilled water. |
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Applications |
VF decreased at ZT12-IP in WT mice only with high dose of GsMTx4 but showed no effects in ClockΔ19/Δ19 mice. GsMTx4 did not affect Uvol in both mice at ZT12-IP. A decrease in Uvol was observed in both mice at ZT0-IP; however, it was unrelated to GsMTx4-IP. The effects of GsMTx4 changed associated with the circadian clock and Piezo1 expression level. |
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References: [1]. Gnanasambandam R, et al. GsMTx4: Mechanism of Inhibiting Mechanosensitive Ion Channels. Biophys J. 2017 Jan 10;112(1):31-45. [2]. Ihara, Tatsuya, et al. "Different effects of GsMTx4 on nocturia associated with the circadian clock and Piezo1 expression in mice." Life Sciences 278 (2021): 119555. |
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| Cas No. | 1209500-46-8 | SDF | |
| 化学名 | Gly-Cys-Leu-Glu-Phe-Trp-Trp-Lys-Cys-Asn-Pro-Asn-Asp-Asp-Lys-Cys-Cys-Arg-Pro-Lys-Leu-Lys-Cys-Ser-Lys-Leu-Phe-Lys-Leu-Cys-Asn-Phe-Ser-Phe | ||
| 分子式 | C185H279N49O45S6 | 分子量 | 4101.89 |
| 溶解度 | Water : 16.67 mg/mL | 储存条件 | -20°C, Sealed storage, away from moisture and light. |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.2438 mL | 1.219 mL | 2.4379 mL |
| 5 mM | 0.0488 mL | 0.2438 mL | 0.4876 mL |
| 10 mM | 0.0244 mL | 0.1219 mL | 0.2438 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
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