GsMTx4
GsMTx4 是一種蜘蛛毒液肽，選擇性地抑制屬于 Piezo 和 TRP 通道家族的陽離子可滲透的機械敏感性通道 (MSCs)。GsMTx4 還可阻斷陽離子選擇性的拉伸激huo通道 (SAC)，減弱溶血磷脂酰膽jian (LPC) 誘導(dǎo)的星形膠質(zhì)細(xì)胞毒性和小膠質(zhì)細(xì)胞反應(yīng)性。GsMTx4 是一種重要的藥理學(xué)工具，可用于鑒定興奮性 MSCs 在正常生理學(xué)和病理學(xué)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[1][2][4].
IC50 & Target：MSCs[1]
體外研究(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].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. |
體內(nèi)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].
MCE 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. |
分子量：4095.83
性狀：Solid
Formula：C185H273N49O45S6
Sequence Shortening
GCLEFWWKCNPNDDKCCRPKLKCSKLFKLCNFSF-NH2 (Disulfide bridge:Cys2-Cys17, Cys9-Cys17, Cys16-Cys30)
運輸條件
Room temperature in continental US; may vary elsewhere.
儲存方式
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)
溶解性數(shù)據(jù)
In Vitro:
H2O : 50 mg/mL (12.21 mM; Need ultrasonic)
DMSO : 50 mg/mL (12.21 mM; Need ultrasonic)
| 濃度溶劑體積質(zhì)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 |
請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備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 儲存時，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。
以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用； 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶
- 1.
請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 1.25 mg/mL (0.31 mM); Clear solution
- 2.
請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1.25 mg/mL (0.31 mM); Clear solution
- 3.
請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 1.25 mg/mL (0.31 mM); Clear solution
參考文獻(xiàn)
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