JNJ 10191584 maleate

Cat. No. 2441

JNJ 10191584 maleate C13H15ClN4O.C4H4O4 [869497-75-6]

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Alternative Name: 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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Varga et al (2005) Inhibitory effects of histamine H4 receptor antagonists on experimental colitis in the rat. Eur.J.Pharmacol. 522 130. PMID: 16213481.

Venable et al (2005) Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine H4 antagonists. J.Med.Chem. 48 8289. PMID: 16366610.

Terzioglu et al (2004) Synthesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H4 receptor antagonists. Bioorg.Med.Chem.Lett. 14 5251. PMID: 15454206.

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