Catalog Number: 2441
Alternate Names: VUF 6002
Chemical Name: 1-[(5-Chloro-1H-benzimidazol-2-yl)carbonyl]-4-methylpiperazine maleate
Biological Activity
Highly selective histamine H4 receptor silent antagonist; binds with high affinity to the human H4 receptor (Ki = 26 nM). > 540-fold selective over the H3 receptor (Ki = 14.1 μM). Inhibits mast cell and eosinophil chemotaxis in vitro with IC50 values of 138 and 530 nM respectively. Orally active in vivo.
Technical Data
  • M.Wt:
    394.81
  • Formula:
    C13H15ClN4O.C4H4O4
  • Solubility:
    Soluble to 50 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Desiccate at RT
  • CAS No:
    869497-75-6
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Inhibitory effects of histamine H4 receptor antagonists on experimental colitis in the rat.
    Varga et al.
    Eur.J.Pharmacol., 2005;522:130
  2. Synthesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H4 receptor antagonists.
    Terzioglu et al.
    Bioorg.Med.Chem.Lett., 2004;14:5251
  3. Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine H4 antagonists.
    Venable et al.
    J.Med.Chem., 2005;48:8289
Citations:

The citations listed below are publications that use Tocris products. Selected citations for JNJ 10191584 maleate include:

1 Citations: Showing 1 - 1

  1. Histamine H3 receptor antagonist OUP-186 attenuates the proliferation of cultured human breast cancer cell lines
    Authors: Tanaka Et al.
    Biochemical and Biophysical Research Communication 2016;480:479

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