Tau-aggregation and neuroinflammation-IN-1

Tau-aggregation and neuroinflammation-IN-1 is a potent tau-aggregation and neuroinflammation inhibitor. Tau-aggregation and neuroinflammation-IN-1 exhibits remarkable inhibitory activities against AcPHF6 and full-length tau aggregation. Tau-aggregation and neuroinflammation-IN-1 has a low cytotoxicity and reduced NO release in LPS-stimulated BV2 cells. Tau-aggregation and neuroinflammation-IN-1 can reverse okadaic acid-induced memory impairment in rats.

Tau-aggregation and neuroinflammation-IN-1 (compound 30) (0-40 μM) reduces the survival of SH-SY5Y cells at 30 μM, and exerts no significant hepatotoxicity in LO2 cells at high concentrations, also exerts no effect on BV2 cell viability at 20 μM^[1].
Tau-aggregation and neuroinflammation-IN-1 (2.5, 5 and 10 μM; 24 hours) retains the anti-inflammatory activity of sodium usnate and inhibits NO release rate by 41% in LPS-stimulated BV2 cells at 10 μM^[1].

Tau-aggregation and neuroinflammation-IN-1 (5 and 10 mg/kg; for 14 days) leads to a substantial improvement of the conventional reference spatial memory and cognitive abilities of OA-induced rats^[1].

References:
[1]. Shi CJ, Peng W, Zhao JH, et al. Usnic acid derivatives as tau-aggregation and neuroinflammation inhibitors. Eur J Med Chem. 2020;187:111961.