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554716 REV-ERBα Agonist, GSK4112 - CAS 1216744-19-2 - Calbiochem

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Tableau de caractéristiques principal

CAS #Empirical Formula
1216744-19-2C₁₈H₂₁ClN₂O₄S

Prix & Disponibilité

Référence DisponibilitéConditionnement Qté Prix Quantité
554716-10MG
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      Description
      OverviewA selective, cell-permeable ligand (EC50 = 250 nM) that acts as a REV-ERBα agonist using a FRET assay. It enhances the recruitment of NCoR peptide to REV-ERBα by up to 70%, and displays no activity towards LRH1, SF1, FXR or ROR, and LXR. Furthermore, it inhibits the promoter activity of Pai1, a known target for REV-ERBα by 30%. This ligand exhibits acute suppression of Bmal1 transcription, and is capable of resetting the molecular rhythm of REV-ERBα-mediated PER2 expression in both Rat-1 lung fibroblasts and on ectopic lung tissues in Luciferase reporter assays. In addition, it is shown to repress the expression of gluconeogenic genes in liver cells and reduce glucose output in primary hepatocytes.
      Catalogue Number554716
      Brand Family Calbiochem®
      SynonymsGSK4112
      References
      ReferencesGrant, D., et al. 2010, ACS Chem. Biol. 5, 925.
      Meng, Q., et al. 2008. Journ. Cell. Sci 121, 3629.
      Product Information
      CAS number1216744-19-2
      FormDark beige solid
      Hill FormulaC₁₈H₂₁ClN₂O₄S
      Chemical formulaC₁₈H₂₁ClN₂O₄S
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Biological Information
      Purity≥95% by HPLC
      Storage and Shipping Information
      Ship Code Shipped with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage -20°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
      Global Trade Item Number
      Référence GTIN
      554716-10MG 04055977193091