CA200843 CellAura fluorescent H3 antagonist [clobenpropit]

(HB7826)

Product overview

  • Name
    CA200843 CellAura fluorescent H3 antagonist [clobenpropit]
  • Short description
    Fluorescent H3 histamine receptor antagonist
  • Biological description
    Fluorescent H3 histamine receptor antagonist (apparent KD values are 7.09, 6.55 and 5.71 for H3, H1 and H2 receptors respectively). Also antagonizes the activity of Histamine, a H1 agonist. Displays no intrinsic activity.
  • Alternative names
    CA200843|H3-633-AN
  • Biological action
    Antagonist
  • Our products in action

Images

Properties

  • Molecular Weight
    848.5
  • Source
    Synthetic
  • Formulation
    Lyophilized film
  • Excitation
    633 nm
  • Emission
    650 nm

Applications

  • Application notes
    For imaging at H3, H2 and H1 receptors use solutions up to 100 nM.
  • Pharmacological validation
    The CellAura fluorescent H3 antagonist [clobenpropit] ligand was shown to antagonize the activity of the agonist, histamine, in a recombinant CHO cell line expressing the human H3 receptor and a cyclic AMP-responsive secreted placental alkaline phosphatase (SPAP) reporter gene, and in similar cell lines expressing either the human H2 or H1 receptors. For the 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 CellAura fluorescent H3 antagonist [clobenpropit] to the basal or forskolin-stimulated cells did not significantly alter basal and stimulated SPAP levels, demonstrating that CellAura fluorescent H3 antagonist [clobenpropit] has no intrinsic agonist activity. To determine the apparent KD for CellAura fluorescent H3 antagonist [clobenpropit] at histamine H3, H2 and H1 receptors, cells were treated with varying concentrations of histamine agonist alone, or in the presence of 1µM CellAura fluorescent H3 antagonist [clobenpropit], 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 CellAura fluorescent H3 antagonist [clobenpropit], compared to the response curve for the agonist alone.

Storing and Using Your Product

  • Storage instructions
    -20°C, protect from light
  • Solubility overview
    Soluble in DMSO
  • Handling
    After thawing individual aliquots for use, we recommend briefly sonicating the sample to ensure it is fully dissolved and the solution is homogeneous. We do not recommend using the product after subjecting it to repetitive freeze-thaw cycles.
  • Shipping conditions
    The product, supplied in a dry form, is stable at ambient temperature for periods of up to a few days and does not require shipping on ice/dry ice.
  • Important
    This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.