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Clobenpropit Fluorescent ligand (Red) (ab118649)

Overview

  • Product nameClobenpropit Fluorescent ligand (Red)
  • Description

    Fluorescent H3 antagonist

  • Alternative names
    H3-633-ANH3/H4-633-AN
  • Biological descriptionFluorescent H3 antagonist (pKD values are 6.55, 5.71 and 7.09 at H1, H2 and H3 respectively). Slight agonist activity in vitro at H2 receptors.

    Excitation wavelength: 633 nm

    Emission wavelength: 650 nm

  • Purity> 97%
  • Properties

  • SelectivityH1: 6.55 | H2: 5.71 | H3: 7.09
  • Excitation633nm
  • Emission650nm
  • Molecular Weight850.00
  • Molecular formulaC44H48BF2N8O3S2
  • Validation notesFor H3, H2 and H1 expressing cell lines, the cyclic AMP-induced expression of SPAP was measured under basal and forskolin-stimulated (maximal) conditions. Addition of ab118649 to the basal or forskolin-stimulated cells did not significantly alter basal and stimulated SPAP levels, demonstrating that ab118649 has no intrinsic agonist activity.
    To determine the apparent KD for ab118649 at histamine H3, H2 and H1receptors, cells were treated with varying concentrations of histamine agonist alone, or in the presence of 1 µM ab118649, and the cyclic AMP-induced expression of SPAP measured.
    The apparent KD at H3, H2 and H1 was calculated from the rightward shift of the agonist response curve in the presence of ab118649, compared to the response curve for the agonist alone.
  • Storage instructionsStore at -20°C. Avoid exposure to light.
  • HandlingFor imaging at H3, H2 and H1 receptors use solutions up to 100 nM in DMSO.
  • Research Areas
  • Applications

    Our Abpromise guarantee covers the use of ab118649 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.
    Fluorescent Cell Imaging Fluorescent Cell Imaging: Use at an assay dependent concentration.
    Receptor Localization Receptor Localization: Use at an assay dependent concentration.

    Clobenpropit Fluorescent ligand (Red) images

    • Left: the ab118649 ligand (100 nm) binding to live CHO cells expressing histamine H3 receptors. Right: Binding blocked by the unlabelled competitor rantidine (10 mM). Nuclei have been counter-stained with Hoechst.
    • To determine the apparent KD for ab118649, cells were treated with varying concentrations of histamine alone, or in the presence of 1 µM ab118649, and the cyclic-AMP induced expression of SPAP measured. The apparent KD was calculated from the rightward shift of the agonist response curve in the presence of ab118649, compared to the response curve for the agonist alone. Antagonist –log KD values for H1= 6.55, H2 =5.71, H3 = 7.09
    • To determine the apparent KD for ab118649, cells were treated with varying concentrations of histamine alone, or in the presence of 1 µM ab118649, and the cyclic-AMP induced expression of SPAP measured. The apparent KD was calculated from the rightward shift of the agonist response curve in the presence of ab118649, compared to the response curve for the agonist alone. Antagonist –log KD values for H1= 6.55, H2 =5.71, H3 = 7.09

    References for Clobenpropit Fluorescent ligand (Red) (ab118649)

    ab118649 has not yet been referenced specifically in any publications.

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