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361567 GSK-3β Inhibitor XXIV - CAS 1005201-24-0 - Calbiochem

361567
  
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      Overview

      Replacement Information

      Key Specifications Table

      CAS #Empirical Formula
      1005201-24-0C₁₈H₁₄N₂O₃S
      Description
      OverviewThe racemic mixture of a cell-permeable oxadiazolo-benzofuranylphenylsulfoxide that inhibits GSK-3β (IC50 = 35, 34, and 140 nM using the racemate, the (S), and the (R) enantiomer, respectively) in a highly selective manner. The eutomer is shown to be orally active in rats and mice and significantly reduce CWS-induced brain tau Thr205 phosphorylation in mice in vivo.
      Catalogue Number361567
      Brand Family Calbiochem®
      Synonyms2-Methyl-5-(3-[4-(methylsulfinyl)phenyl)-1-benzofuran-5-yl)-1,3,4-oxadiazole, Racemic
      References
      ReferencesSaitoh, M., et al. 2009. J. Med. Chem. 52, 6270.
      Product Information
      CAS number1005201-24-0
      FormWhite solid
      Hill FormulaC₁₈H₁₄N₂O₃S
      Chemical formulaC₁₈H₁₄N₂O₃S
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥98% 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 at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      GSK-3β Inhibitor XXIV - CAS 1005201-24-0 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Saitoh, M., et al. 2009. J. Med. Chem. 52, 6270.
      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.

      Revision26-March-2012 JSW
      Synonyms2-Methyl-5-(3-[4-(methylsulfinyl)phenyl)-1-benzofuran-5-yl)-1,3,4-oxadiazole, Racemic
      DescriptionThe racemic mixture of a cell-permeable oxadiazolo-benzofuranylphenylsulfoxide that inhibits GSK-3β (IC50 = 35, 34, and 140 nM using the racemate, the (S), and the (R) enantiomer, respectively) in a highly selective manner as evidenced by its eutomer's inability to inhibit 10 other serine/threonine and 12 other tyrosine kinases even at concentrations as high as 10 µM. Reported to exhibit good aqueous solubility (38 µg racemate/ml pH 6.8 buffer) and pharmacokinetic properties, being orally active in both rats and mice in vivo (Plasma AUC0-24h = 1380.6 and 457 ng•h/mL, respectively; 3 mg eutomer/kg via p.o.). The eutomer is also shown to be blood-brain-permeant in mice (brain AUC0-24h = 734 ng•h/mL; 3 mg/kg via p.o.) and oral dosing 30 min prior to CWS (cold water stress; 4 min below-neck inversion in 1-2 °C water) is demonstrated to reduce brain tau Thr205 phosphorylation (by 35%; 10 min post CWS) in mice in vivo.
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1005201-24-0
      Chemical formulaC₁₈H₁₄N₂O₃S
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesSaitoh, M., et al. 2009. J. Med. Chem. 52, 6270.