Tau-aggregation and neuroinflammation-IN-1

• CAT Number: I043835
• CAS Number: 2175953-98-5
• Molecular Formula: C25H20N2O7
• Molecular Weight: 460.44
• Purity: ≥95%
• Synonyms: 4-[(4aR)-8-acetyl-5,7-dihydroxy-3,4a,6-trimethyl-4-oxo-[1]benzofuro[3,2-f]indazol-1-yl]benzoic acid
• InChI: InChI=1S/C25H20N2O7/c1-10-20(29)18(12(3)28)22-19(21(10)30)25(4)16(34-22)9-15-17(23(25)31)11(2)26-27(15)14-7-5-13(6-8-14)24(32)33/h5-9,29-30H,1-4H3,(H,32,33)/t25-/m0/s1
• InChIKey: AKUILIKFHHXNNL-VWLOTQADSA-N
• SMILES: CC1=C(C(=C2C(=C1O)C3(C(=CC4=C(C3=O)C(=NN4C5=CC=C(C=C5)C(=O)O)C)O2)C)C(=O)C)O

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[1].
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].

Reference

[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.
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