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].
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