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580222 Tau Aggregation Inhibitor, ATPZ, Cpd16 - Calbiochem

580222
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Overview

Replacement Information

Products

Catalogue NumberPackaging Qty/Pack
580222-10MG Glass bottle 10 mg
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
Catalogue Number GTIN
580222-10MG 04055977265453

Documentation

Tau Aggregation Inhibitor, ATPZ, Cpd16 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

Tau Aggregation Inhibitor, ATPZ, Cpd16 - Calbiochem Certificates of Analysis

TitleLot Number
580222

References

Reference overview
Ballatore, C., et al. 2010. J. Med. Chem. 53, 3739.
Data Sheet

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.