General description
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.
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Ballatore, C., et al. 2010. J. Med. Chem.53, 3739.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Molecular Weight: 360.82. Empirical Formula: C16H13ClN4O2S. Assay: ≥. 95% (HPLC). Quality Level: 100. form: powder. manufacturer/tradename: Calbiochem®. . storage condition: OK to freeze. color: orange. solubility: DMSO: 50 . mg/mL. shipped in: wet ice. storage temp.: −. 20°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 2. Flash Point(F): Not applicable. Flash Point(C): Not applicable.- UPC:
- 12352200
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 580222-10MG