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TRx0237 is an inhibitor of tau aggregation.1 It inhibits tau-tau binding (IC50 = 238 µM) and tau aggregation in 3T6H cells expressing human tau (EC50 = 0.19 µM). TRx0237 (5 and 15 mg/kg) increases hippocampal acetylcholine (ACh) and synaptophysin levels, as well as increases mitochondrial complex IV activity, decreases tau pathology, and reverses deficits in spatial learning in the L1 transgenic mouse model of Alzheimer’s disease.2
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1. Cellular models of aggregation-
2. Mechanisms of anticholinesterase interference with tau aggregation inhibitor activity in a tau-