182707 AhR Antagonist III, GNF351 - Calbiochem

182707
  
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₄H₂₅N₇
      Description
      OverviewA cell-permeable purine compound that acts as a high-affinity aryl hydrocarbon receptor (AhR) antagonist (IC50 = 62 nM in mouse liver cytosol expressing humanized AhR) and lacks any agonist activity even at higher doses. Reportedly binds with high affinity to the ligand-binding pocket of AhR and blocks the binding of an array of exogenous and endogenous ligands. Shown to non-covalently interact with Ser317, His291, and Ser365 in human and with Ser311, His285, and Ser359 in mouse AhR. Represses AhR transcriptional activity via the dioxin response element (DRE)-dependent and independent mediated responses in human and mouse cells (IC50 = 8.5 nM in HepG2 40/6 cells).
      Catalogue Number182707
      Brand Family Calbiochem®
      SynonymsN-(2-(3H-Indol-3-yl)ethyl)-9-isopropyl-2-(5-methyl-3-pyridyl)-7H-purin-6-amine, N-(2-(1H-Indol-3-yl)ethyl)-9-isopropyl-2-(5-methylpyridin-3-yl)-9H-purin-6-amine
      References
      ReferencesSmith, K.J., et al. 2011. J. Pharmacol. Exp. Ther. 338, 318.
      Product Information
      FormOff-white solid
      Hill FormulaC₂₄H₂₅N₇
      Chemical formulaC₂₄H₂₅N₇
      Structure formula ImageStructure formula Image
      Applications
      ApplicationAhR Antagonist III, GNF351, is a cell-permeable, high-affinity aryl hydrocarbon receptor (AhR) antagonist (IC50 = 62 nM in mouse liver cytosol expressing humanized AhR).
      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

      AhR Antagonist III, GNF351 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      AhR Antagonist III, GNF351 - Calbiochem Certificates of Analysis

      TitleLot Number
      182707

      References

      Reference overview
      Smith, K.J., et al. 2011. J. Pharmacol. Exp. Ther. 338, 318.
      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.

      Revision06-February-2013 JSW
      SynonymsN-(2-(3H-Indol-3-yl)ethyl)-9-isopropyl-2-(5-methyl-3-pyridyl)-7H-purin-6-amine, N-(2-(1H-Indol-3-yl)ethyl)-9-isopropyl-2-(5-methylpyridin-3-yl)-9H-purin-6-amine
      DescriptionA cell-permeable purine compound that acts as a high-affinity aryl hydrocarbon receptor (AhR) antagonist (IC50 = 62 nM in mouse liver cytosol expressing humanized AhR) and lacks any agonist activity even at higher doses. Reportedly binds with high affinity to the ligand-binding pocket of AhR and blocks the binding of an array of exogenous and endogenous ligands. Shown to non-covalently interact with Ser317, His291, and Ser365 in human and with Ser311, His285, and Ser359 in mouse AhR. Represses AhR transcriptional activity via the dioxin response element (DRE)-dependent and independent mediated responses in human and mouse cells (IC50 = 8.5 nM in HepG2 40/6 cells).
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₄H₂₅N₇
      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
      ReferencesSmith, K.J., et al. 2011. J. Pharmacol. Exp. Ther. 338, 318.