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580222 Tau Aggregation Inhibitor, ATPZ, Cpd16 - Calbiochem

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Synonyme: 5-amino-3-(4-chlorophenyl)-N-cyclopropyl-4-oxo-3,4-dihydrothieno[3,4-d]pyridazine-1-carboxamide

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580222
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Preis & Verfügbarkeit

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580222-10MG
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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
      Applications
      Biological Information
      Purity≥95% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      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.
      Packaging Information
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Bestellnummer GTIN
      580222-10MG 04055977265453

      Documentation

      Tau Aggregation Inhibitor, ATPZ, Cpd16 - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      Tau Aggregation Inhibitor, ATPZ, Cpd16 - Calbiochem Analysenzertifikate

      TitelChargennummer
      580222

      Literatur

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

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision28-February-2011 RFH
      Synonyms5-amino-3-(4-chlorophenyl)-N-cyclopropyl-4-oxo-3,4-dihydrothieno[3,4-d]pyridazine-1-carboxamide
      DescriptionA 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.
      FormOrange powder
      Chemical formulaC₁₆H₁₃ClN₄O₂S
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (50 mg/ml)
      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.
      Toxicity Standard Handling
      ReferencesBallatore, C., et al. 2010. J. Med. Chem. 53, 3739.