Cayman AA147

AA147 is an endoplasmic reticulum (ER) proteostasis regulator.^1,2,3 It activates an activating transcription factor 6-dependent (ATF6-dependent) ER stress response element reporter and antioxidant response element reporter in HT22 hippocampal cells (EC₅₀s = 3.6 and 3.92 µM, respectively) and protects against glutamate-induced cytotoxicity and prevents increases in reactive oxygen species (ROS) in HT22 cells when used at a concentration of 10 µM.¹ AA147 (10 µM) reduces cell death induced by the unfolded protein response (UPR) activator tunicamycin and increases ER-associated protein degradation (ERAD) in neonatal rat ventricular myocytes.² It reduces the myocardial, renal, and cerebral infarct size as a percentage of the area at risk in mouse models of ischemia-reperfusion injury induced by left anterior descending coronary artery (LAD) ligation, renal portal system occlusion, or middle cerebral artery occlusion (MCAO), respectively, when administered at a dose of 2 mg/kg. AA147 also prevents the production of non-structural protein 5 (NS5) in dengue virus-infected Huh7 cells (IC₅₀ = ~1 µM).³

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