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Aminopotentidine Fluorescent ligand (Red) (ab118175)

Overview

  • Product nameAminopotentidine Fluorescent ligand (Red)
  • Description

    Fluorescent H2 antagonist

  • Alternative names
    H2-633-AN
  • Biological descriptionFluorescent H2 antagonist (pKD values are 8.94 and 7.30 at H2 and H3 receptors respectively). No intrinsic agonist activity in vitro. Wide range of applications which include localizing receptor distribution in tissues and cells, and live-cell imaging of receptor kinetics.

    Excitation wavelength: 633 nm

    Emission wavelength: 650 nm

  • Purity> 97%
  • Properties

  • PharmacophoreAminopotentidine-derivative
  • SelectivityH1: >6 | H2: 8.94 | H3: 7.30
  • Excitation633nm
  • Emission650nm
  • Molecular Weight904.00
  • Molecular formulaC48H56BF2N9O4S
  • Validation notesFor the H2 and H3 expressing cell lines, the cyclic AMP-induced expression of SPAP was measured under basal and forskolin stimulated (maximal) conditions. Addition of ab118175 to the basal or forskolin-stimulated cells did not significantly alter basal and stimulated SPAP levels, demonstrating that ab118175 has no intrinsic agonist activity.
    To determine the KD for ab118175 at histamine H2 and H3 receptors, cells were treated with concentrations of histamine agonist alone, or in the presence of 1 µM ab118175, and the cyclic AMP-induced expression of SPAP measured.
    The KD at H2 was calculated from the shift of the agonist response curve in the presence of ab118175, compared to the response curve for the agonist alone.
  • Storage instructionsStore at -20°C. Avoid exposure to light.
  • HandlingFor imaging at the H2 or H3 receptor use solutions up to 100 nM in DMSO.
  • Research Areas
  • Applications

    Our Abpromise guarantee covers the use of ab118175 in the following tested applications.

    The application notes include recommended starting dilutions; optimal dilutions/concentrations should be determined by the end user.

    Application Notes
    Small Molecule Fluorescent Optical Detection Small Molecule Fluorescent Optical Detection: Use at an assay dependent concentration.
    Receptor Localization Receptor Localization: Use at an assay dependent concentration.
    Fluorescent Cell Imaging Fluorescent Cell Imaging: Use at an assay dependent concentration.

    Aminopotentidine Fluorescent ligand (Red) images

    • Left: ab118175 ligand (30 nM) binding to CHO cells expressing histamine H2 receptors. Right: Binding blocked by the unlabelled competitor ranitidine (10 µM). Nuclei have been counter-stained with Hoechst.
    • To determine the apparent KD for ab118175 at histamine H2 receptor, cells were treated with varying concentrations of histamine agonist alone, or in the presence of 1 µM ab118175, and the cyclic AMP-induced expression of SPAP measured.
      The apparent KD at H2 was calculated from the rightward shift of the agonist response curve in the presence of ab118175, compared to the response curve for the agonist alone. KD value for H2 was found to be 8.94 Antagonist -log KD.
    • To determine the apparent KD for ab118175 at histamine H3 receptor, cells were treated with varying concentrations of histamine agonist alone, or in the presence of 1 µM ab118175, and the cyclic AMP-induced expression of SPAP measured.
      The apparent KD at H3 was calculated from the rightward shift of the agonist response curve in the presence of ab118175, compared to the response curve for the agonist alone. The KD for ab118175 was found to be 7.3 Antagonist-log KD

    References for Aminopotentidine Fluorescent ligand (Red) (ab118175)

    ab118175 has not yet been referenced specifically in any publications.

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