182707 | AhR Antagonist III, GNF351 - Calbiochem

182707
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₄H₂₅N₇

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      182707-10MG
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          Glass bottle 10 mg
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          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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.