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440165 LXRα/β Agonist - CAS 264206-85-1 - Calbiochem

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Synonyme: 3-((4-Methoxyphenyl)amino)-4-phenyl-1-(phenylmethyl)-1H-pyrrole-2,5-dione

Primary Target: A potent and specific liver X receptor (LXR) dual agonist
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      Übersicht

      Replacement Information

      Key Spec Table

      CAS #Empirical Formula
      264206-85-1C₂₄H₂₀N₂O₃
      Description
      Overview

      This product has been discontinued.



      A cell-permeable maleimide analog that acts as a potent and specific liver X receptor (LXR) dual agonist (EC50 = 50 nM and 40 nM for the recruitment of SRC1 to LXRα and LXRβ, respectively). Displays >50-fold selectivity for LXR over a panel of nuclear receptors, including FXR, PPARα/γ/δ, PXR, AR, ERα/β, GR, and PR. Upregulates ABCA1-dependent transcriptional activity (EC50 = 80 nM) and inhibits LPS-stimulated secretion of the proinflammatory cytokine, IL-6, in THP-1 cells.
      Catalogue Number440165
      Brand Family Calbiochem®
      Synonyms3-((4-Methoxyphenyl)amino)-4-phenyl-1-(phenylmethyl)-1H-pyrrole-2,5-dione
      References
      ReferencesJaye, M.C., et al. 2005. J. Med. Chem. 48, 5419.
      Product Information
      CAS number264206-85-1
      ATP CompetitiveN
      FormOrange solid
      Hill FormulaC₂₄H₂₀N₂O₃
      Chemical formulaC₂₄H₂₀N₂O₃
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetA potent and specific liver X receptor (LXR) dual agonist
      Primary Target IC<sub>50</sub>EC50 = 50 nM and 40 nM for the recruitment of SRC1 to LXRα and LXRβ, respectively
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableN
      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 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 1 year at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Bestellnummer GTIN
      440165 0

      Documentation

      LXRα/β Agonist - CAS 264206-85-1 - Calbiochem Analysenzertifikate

      TitelChargennummer
      440165

      Literatur

      Übersicht
      Jaye, M.C., et al. 2005. J. Med. Chem. 48, 5419.
      Datenblatt

      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.

      Revision13-April-2011 RFH
      Synonyms3-((4-Methoxyphenyl)amino)-4-phenyl-1-(phenylmethyl)-1H-pyrrole-2,5-dione
      DescriptionA cell-permeable maleimide analog that acts as a potent and specific liver X receptor (LXR) dual agonist (EC50 = 50 nM and 40 nM for the recruitment of SRC1 to LXRα and LXRβ, respectively). Displays >50-fold selectivity for LXR over a panel of nuclear receptors, including FXR, PPARα/γ/δ, PXR, AR, ERα/β, GR, and PR. Upregulates ABCA1-dependent transcriptional activity (EC50 = 80 nM) and inhibits LPS-stimulated secretion of the proinflammatory cytokine, IL-6, in THP-1 cells.
      FormOrange solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number264206-85-1
      Chemical formulaC₂₄H₂₀N₂O₃
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (200 mg/ml) or Methanol (100 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 year at -20°C.
      Toxicity Standard Handling
      ReferencesJaye, M.C., et al. 2005. J. Med. Chem. 48, 5419.