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

361567
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₈H₁₄N₂O₃S 1005201-24-0

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      361567-5MG
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          Glass bottle 5 mg
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          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
          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

          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 +2°C to +8°C
          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.
          Toxicity Standard Handling
          ReferencesSaitoh, M., et al. 2009. J. Med. Chem. 52, 6270.