JNJ 10191584 maleate
Cat. No. 2441
Alternative Name: VUF 6002
Chemical Name: 1-[(5-Chloro-1H-benzimidazol-2-yl)c
Biological ActivityHighly 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.
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 Datasheet
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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Citations are publications that use Tocris products. Selected citations for JNJ 10191584 maleate include:
Tanaka et al (2016) Histamine H3 receptor antagonist OUP-186 attenuates the proliferation of cultured human breast cancer cell lines Biochemical and Biophysical Research Communication 480 479. PMID: 27773822.
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