JNJ 10191584 | Histamine Receptors | Selective H4 Receptor Antagonist; Orally Active | VUF 6002 | JNJ10191584

Category:

7TM Receptors

Histamine Receptors

H3 and H4 Receptors

Antagonists

Cat.No.

Product Name

2441

JNJ 10191584 maleate

Alternative name(s):

VUF 6002

JNJ 10191584 C13H15ClN4O.C4H4O4 1-[(5-Chloro-1H-benzimidazol-2-yl)carbonyl]-4-methylpiperazine maleate

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JNJ 10191584

Chemical Name: 1-[(5-Chloro-1H-benzimidazol-2-yl)carbonyl]-4-methylpip erazine maleate

Biological Activity:

Highly selective histamine H₄ receptor silent antagonist; binds with high affinity to the human H₄ receptor (K_i = 26 nM) and is > 540-fold selective over the H₃ receptor (K_i = 14.1 μM). In vitro, inhibits mast cell and eosinophil chemotaxis with IC₅₀ values of 138 and 530 nM respectively. Orally active in vivo.

Technical Data:

M.Wt:	394.81
Formula:	C₁₃H₁₅ClN₄O.C₄H₄O₄
Storage:	Desiccate at RT
Solubility:	Soluble to 50 mM in DMSO
Purity:	>99%
CAS No:	[869497-75-6]

Resources:

Certificate of Analysis / MSDS:

Certificate of Analysis: View current batch

Product/Material Safety Data Sheet: View current batch

References:

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. Venable et al (2005) Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine H₄antagonists. J.Med.Chem. 48 8289. Varga et al (2005) Inhibitory effects of histamine H₄ receptor antagonists on experimental colitis in the rat. Eur.J.Pharmacol. 522 130.

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Keywords: JNJ 10191584, Histamine Receptors, Selective H4 Receptor Antagonist; Orally Active, VUF 6002, JNJ10191584, Tocris Bioscience

Literature in this Area

Scientific Reviews

Histamine Receptors
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