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AA147

CAS No. : 393121-74-9

MCE 国际站：AA147

产品活性：AA147 是一种内质网 (ER) 蛋白稳态调节剂。AA147 可通过选择性激活未折叠蛋白反应的 ATF6 臂以及激活 NRF2 氧化应激反应来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。AA147 还可重新平衡 XBP1s 在体内的表达，并诱导运动神经元存活基因的表达并保护脊柱运动神经元。

研究领域：Cell Cycle/DNA Damage  |  Metabolic Enzyme/Protease  |  Immunology/Inflammation  |  NF-κB

作用靶点：ATF6  |  Reactive Oxygen Species

In Vitro: AA147 (20-0.078 μM (dilution in half); 6 or 16 h) protects against glutamate-induced oxidative toxicity in HT22 cells by decreasing the reactive oxygen species (ROS)-associated damage.
AA147 (10 μM; 16 h) induces NRF2-dependent upregulation of oxidative stress response genes in HT22 cells.
AA147 (10 μM; 16 h) covalently modifies KEAP1 to promote NRF2 activation in HT22 cells.
AA147 (5, 10, 15 μM; 4, 8, 16, 24, 48 h) induces ATF6 activation and upregulates phosphorylation of cofilin in BPAEC.
AA147 (10 μM; 24 h) reduces LPS-induced endothelial barrier disruption in BPAEC.
AA147 (5, 10 μM; 135 h) enhances lung endothelial barrier integrity.

In Vivo: AA147 (intrathecal injection; single for 3 days) can rebalance XBP1s expression in severe SMA-like mice by activating ATF6, and also induce survival motor neuron expression and spinal motorneuron protection.

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