580222

Tau Aggregation Inhibitor, ATPZ, Cpd16

• Synonym(e): Tau Aggregation Inhibitor, ATPZ, Cpd16, 5-amino-3-(4-chlorophenyl)-N-cyclopropyl-4-oxo-3,4-dihydrothieno[3,4-d]pyridazine-1-carboxamide
• Empirische Formel (Hill-System): C₁₆H₁₃ClN₄O₂S
• Molekulargewicht: 360.82
• NACRES: NA.77
• UNSPSC Code: 12352200
• Assay: ≥95% (HPLC)
• Form: powder
• Storage condition: OK to freeze

Eigenschaften

• assay: ≥95% (HPLC)
• Quality Segment: 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

Beschreibung

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.

Preparation Note

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

Disclaimer

Toxicity: Standard Handling (A)

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable