Tau Aggregation Inhibitor, ATPZ, Cpd16

A water soluble (32 µM in water) BBB-permeable ATPZ (aminothienopyridazine) tau aggregation inhibitor that exhibited IC₅₀ of 8.1 µM in a heparin-induced tau assembly assay (monitored by thioflavine-T binding and fluorescence), and was further validated in vitro to reduce tau fibril formation (tau fragment K18PL, and full length tau40) by >50% in sedimentation assays. It also displayed very good B/P ratio (1.6) in a mice full PK study with good oral bioavailability and good metabolic stability. No cytotoxicity was observed at up to 100 µM in HEK-293 cells.

A water soluble (32uM in water) BBB-permeable ATPZ (aminothienopyridazine) tau aggregation inhibitor that exhibited IC50 of 8.1uM in a heparin-induced tau assembly assay (monitored by thioflavine-T binding and fluorescence), and was further validated in vitro to reduce tau fibril formation (tau fragment K18PL, and full length tau40) by >50% in sedimentation assays. It also displayed very good B/P ratio (1.6) in a mice full PK study with good oral bioavailability and good metabolic stability. No cytotoxicity was observed at up to 100uM in HEK-293 cells.

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Ballatore, C., et al. 2010. J. Med. Chem.53, 3739.

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