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580222 Tau Aggregation Inhibitor, ATPZ, Cpd16 - Calbiochem

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580222-10MG
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      Glass bottle 10 mg
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      Description
      OverviewA 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.
      Catalogue Number580222
      Brand Family Calbiochem®
      Synonyms5-amino-3-(4-chlorophenyl)-N-cyclopropyl-4-oxo-3,4-dihydrothieno[3,4-d]pyridazine-1-carboxamide
      References
      ReferencesBallatore, C., et al. 2010. J. Med. Chem. 53, 3739.
      Product Information
      FormOrange powder
      Hill FormulaC₁₆H₁₃ClN₄O₂S
      Chemical formulaC₁₆H₁₃ClN₄O₂S
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Biological Information
      Purity≥95% by HPLC
      Storage and Shipping Information
      Ship Code Shipped with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage -20°C
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Global Trade Item Number
      Catalogue Number GTIN
      580222-10MG 04055977265453