516571 | PPAR Agonist IX, GQ-16 - Calbiochem

516571
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₉H₁₆BrNO₃S

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      516571-25MG
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          Glass bottle 25 mg
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          Description
          OverviewA cell-permeable thiazolidinedione that acts as a PPARγ-selective agonist (Ki = 160 nM) and blocks Cdk-5-mediated Ser273 phosphorylation by stabilizing PPARγ β-sheet structure, exhibiting no detectable activity towards PPARα, PPARδ, or RXRα. Although a weaker PPAPγ agonist than Thiazolidinediones (TZDs) family rosiglitazone (Cat. No. 557366; Max. fold of transactivation induction = 8.57 and 24.8 with 10 µM respective compound in U-937 reporter assays), GQ-16 can be safely administered at a higher dosage (20 mg/kg/day; oral gavage) in mice to achieve similar in vivo efficacy as rosiglitazone (4 mg/kg/day; o.g.) without adverse side effects commonly seen with TZDs.
          Catalogue Number516571
          Brand Family Calbiochem®
          Synonyms(Z)-5-(5-Bromo-2-methoxybenzylidene)-3-(4-methyl-benzyl)-thiazolidine-2,4-dione
          References
          ReferencesAmato, A.A., et al. 2012. J. Biol. Chem. 287, 28169.
          Product Information
          FormPale yellow solid
          Hill FormulaC₁₉H₁₆BrNO₃S
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary TargetPPARγ
          Purity≥99% by HPLC
          Physicochemical Information
          Cell permeableY
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          Safety Information
          Product Usage Statements
          Storage and Shipping Information
          Ship Code Ambient Temperature Only
          Toxicity Harmful
          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) 

          Certificates of Analysis

          TitleLot Number
          516571

          References

          Reference overview
          Amato, A.A., et al. 2012. J. Biol. Chem. 287, 28169.
          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.

          Revision24-October-2012 JSW
          Synonyms(Z)-5-(5-Bromo-2-methoxybenzylidene)-3-(4-methyl-benzyl)-thiazolidine-2,4-dione
          DescriptionA cell-permeable thiazolidinedione that acts as a PPARγ-selective agonist (Ki = 160 nM) and blocks Cdk-5-mediated Ser273 phosphorylation by stabilizing PPARγ β-sheet structure, exhibiting no detectable activity towards PPARα, PPARδ, or RXRα. Although a weaker PPAPγ agonist than Thiazolidinediones (TZDs) family rosiglitazone (Cat. No. 557366; Max. fold of transactivation induction = 8.57 and 24.8 with 10 µM respective compound in U-937 reporter assays), GQ-16 can be safely administered at a higher dosage (20 mg/kg/day; oral gavage) in mice to achieve similar in vivo efficacy as rosiglitazone (4 mg/kg/day; o.g.) in reversing high fat diet-induced insulin signaling defects without adverse side effects commonly seen with TZDs.such as edema and weight gain commonly seen with TZDs.
          FormPale yellow solid
          Intert gas (Yes/No) Packaged under inert gas
          Structure formulaStructure formula
          Purity≥99% 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 6 months at -20°C.
          Toxicity Harmful
          ReferencesAmato, A.A., et al. 2012. J. Biol. Chem. 287, 28169.