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编 号:F761072
分子式:C200H312N62O57S6
分子量:4689.39
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100μg
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生物活性:
Psalmotoxin 1 (PcTx1) is a protein toxin that can bind at subunit-subunit interfaces of acid-sensing ion channel 1a (ASIC1a). Psalmotoxin 1 is a potent and slective ASIC1a inhibitor (IC50: 0.9 nM) by increasing the apparent affinity for H+ of ASIC1a. Psalmotoxin 1 can induce cell apoptosis, also inhibits cell migration, proferliration and invasion of cancer cells. Psalmotoxin 1 can be used in the research of cancers, or neurological disease.

体内研究:
Psalmotoxin 1 (icv,1 ng/kg,单次剂量) 通过直接抑制 ASIC1a 在有意识的中风模型中发挥神经保护作用。Psalmotoxin 1 (尾静脉注射,10 ng/kg,每日一次,持续 7 天) 抑制乳腺癌小鼠模型的肿瘤生长。Animal Model:Male spontaneously hypertensive rats (SHR)
Dosage:1 ng/kg, a single dose.
Administration:Intracerebroventricular (i.c.v.) injection
Result:Reduced cortical and striatal infarct volumes measured 72 h post-stroke.Reduced the severity of motor deficit at 1 and 3 days after stroke compared to control rats. Displayed an anti-apoptotic effect in the occluded hemisphere (reduced stroke-induced caspase-3 positive cells).
Animal Model:Female nude BALB/C mice (orthotopic implantation, MCF-7 and MDA-MB-231 cells)
Dosage:10 ng/kg, daily for 7 days.
Administration:Tail vein injection
Result:Inhibited breast tumor growth.

体外研究:
Psalmotoxin 1 (20 nM,125 s) 通过显著改变稳态脱敏曲线以降低 H+ 浓度来抑制 ASIC1a 电流。Psalmotoxin 1 (30 nM) 与 Ca2+ 竞争结合 ASIC1a 通道。 Psalmotoxin 1 (100 或 200 ng,24-72 小时) 显著减弱 MCF-7 和 MDA-MB-231 细胞的迁移、增殖和侵袭。 Psalmotoxin 1 (100 ng/mL,24 h) 显著抑制酸诱导的增加参与细胞内钙和 LDH 释放,诱导髓核细胞 (NPC) 细胞凋亡和细胞周期停滞。
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