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。

AA147 is a endoplasmic reticulum (ER) proteostasis regulator. AA147 promotes protection against oxidative damage in neuronal cells and prevents endothelial barrier dysfunction by activating ATF6 arm (selectively) of the unfolded protein response (UPR) and the NRF2 oxidative stress response. AA147 can rebalances XBP1s expression in vivo, and also induces survival motor neuron (SMN) expression and spinal motorneuron (MN) protection.

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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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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[1]. Rosarda JD, et al. Metabolically Activated Proteostasis Regulators Protect against Glutamate Toxicity by Activating NRF2. ACS Chem Biol. 2021 Dec 17;16(12):2852-2863.
[2]. Kubra KT, et al. Activating transcription factor 6 protects against endothelial barrier dysfunction. Cell Signal. 2022 Aug 4;99:110432.

In Vitro: DMSO : 50 mg/mL (195.84 mM; Need ultrasonic)配制储备液