AA147是一种内质网 (ER) 蛋白稳态调节剂,选择性激活未折叠蛋白反应的 ATF6 臂,同时激活 NRF2 氧化应激反应,促进对神经元细胞氧化损伤的保护,并防止内皮屏障功能失调。
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描述 | AA147 is an endoplasmic reticulum (ER) proteostasis regulator. It enhances protection against oxidative damage in neuronal cells and prevents endothelial barrier dysfunction by selectively activating the ATF6 arm of the unfolded protein response (UPR) and the NRF2 oxidative stress response. In vivo, AA147 rebalances XBP1s expression and induces survival motor neuron (SMN) expression, thereby protecting spinal motor neurons [1][2][3][4]. |
体内研究 | AA147 (intrathecal injection; single for 3 days) rebalances XBP1s expression in severe SMA-like mice by activating ATF6. Additionally, it induces expression of survival motor neuron and protects spinal motor neurons [3]. |
体外研究 | AA147 (20-0.078 μM (dilution in half); 6 or 16 h) shields against glutamate-induced oxidative toxicity in HT22 cells by reducing reactive oxygen species (ROS)-associated damage [1]. AA147 (10 μM; 16 h) triggers NRF2-dependent upregulation of oxidative stress response genes in HT22 cells [1]. AA147 (10 μM; 16 h) covalently alters KEAP1 to enhance NRF2 activation in HT22 cells [1]. AA147 (5, 10, 15 μM; 4, 8, 16, 24, 48 h) triggers ATF6 activation and increases phosphorylation of cofilin in BPAEC [2]. AA147 (10 μM; 24 h) mitigates LPS-induced endothelial barrier disruption in BPAEC [2]. AA147 (5, 10 μM; 135 h) improves lung endothelial barrier integrity [2]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
3.92mL 0.78mL 0.39mL |
19.58mL 3.92mL 1.96mL |
39.17mL 7.83mL 3.92mL |
CAS号 | 393121-74-9 |
分子式 | C16H17NO2 |
分子量 | 255.312 |
别名 | |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,Room Temperature |
溶解方案 |
DMSO: 50 mg/mL(195.84 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的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
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动物实验配方 |