344355 | Foxo1 Inhibitor, AS1842856 - Calbiochem

344355
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₈H₂₂FN₃O₃

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      344355-10MG
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable oxodihydroquinoline that preferentially inhibits the transcription activity of Forkhead box O family member Foxo1 (IC50 = 33 nM) over that of the functionally related Foxo3a and Foxo4 (70%, 20%, and 3% inhibition, respectively, in HepG2-based reporter assays; [AS184256] = 100 nM) via direct binding of the active Foxo1, but not the Ser256-phosphorylated/inactive form of Foxo1. Shown to inhibit gluconeogenesis in rat heptoma Fao cultures (IC50 = 43 nM against glucose production) in vitro and in liver of both non-diabetic and diabetic mice during a 26-hour fasting period (100 mg/kg/8 h p.o.) in vivo. Also available as a 50 mM solution in DMSO (Cat. No. 506081).
          Catalogue Number344355
          Brand Family Calbiochem®
          Synonyms5-Amino-7-(cyclohexylamino)-1-ethyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
          References
          ReferencesNagashima, T., et al. 2010. Mol. Pharmacol. 78, 961.
          Product Information
          FormOff-white to tan to yellow solid
          Hill FormulaC₁₈H₂₂FN₃O₃
          Chemical formulaC₁₈H₂₂FN₃O₃
          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 Regulatory Review
          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 3 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) 

          Certificates of Analysis

          TitleLot Number
          344355

          References

          Reference overview
          Nagashima, T., et al. 2010. Mol. Pharmacol. 78, 961.
          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.

          Revision09-September-2016 JSW
          Synonyms5-Amino-7-(cyclohexylamino)-1-ethyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
          DescriptionA cell-permeable oxodihydroquinoline that preferentially inhibits the transcription activity of Forkhead box O family member Foxo1 over that of the functionally related Foxo3a and Foxo4 (70%, 20%, and 3% inhibition, respectively, in HepG2-based reporter assays; [AS184256] = 100 nM) in a dose-dependent manner (IC50 = 33 nM) via direct binding of the non-Ser256-phosphorylated/active Foxo1, but not the Ser256-phosphorylated/inactive form of Foxo1. Shown to inhibit gluconeogenesis in rat heptoma Fao cultures (IC50 = 37 and 130 nM against PEPCK and G6Pase mRNA level; IC50 = 43 nM against glucose production) in vitro and in murine liver of both normoglycemic ICR mice (60% and 45% inhibition of hepatic G6Pase and PEPCK mRNA level, respectively; three 100 mg/kg p.o. dosages at 0, 12, 24 h) and diabetic db/db mice (86%, 70%, 56%, 48%, 35%, and 31% inhibition of hepatic G6Pase, ABCG8, ABCG5, PEPCK, IL-1β, and apoCIII mRNA level, respectively; three 100 mg/kg p.o. dosages at 0, 12, 24 h) during a 26-hour fasting period in vivo.
          FormOff-white to tan to yellow solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₈H₂₂FN₃O₃
          Structure formulaStructure formula
          Purity≥98% by HPLC
          SolubilityDMSO (5 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 3 months at -20°C.
          Toxicity Regulatory Review
          ReferencesNagashima, T., et al. 2010. Mol. Pharmacol. 78, 961.