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JNJ 10191584 maleate

Chemical Structure : JNJ 10191584 maleate

CAS No.: 869497-75-6

JNJ 10191584 maleate

Catalog No.: PC-20925Not For Human Use, Lab Use Only.

JNJ-10191584 (VUF6002) maleate is a potent, highly selective, orally active histamine H(4) receptor antagonist with binding Ki of 26 nM, 540-fold selectivity to H4 receptor over H3 receptor.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

JNJ-10191584 (VUF6002) maleate is a potent, highly selective, orally active histamine H(4) receptor antagonist with binding Ki of 26 nM, 540-fold selectivity to H4 receptor over H3 receptor.
JNJ-10191584 (VUF6002) shows inhibitory effects to chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively.
JNJ 10191584 (10-100 mg/kg p.o., b.i.d.) caused a dose-dependent reduction in macroscopic damage, inhibition of the TNBS-provoked elevation of both colonic myeloperoxidase and tumour necrosis factor-alpha (TNF-alpha), and a reduction in the histologically assessed increase in mucosal and submucosal thickness and neutrophil infiltration.

Physicochemical Properties

M.Wt 394.81
Formula C17H19ClN4O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(5-chloro-1H-benzo[d]imidazol-2-yl)(4-methylpiperazin-1-yl)methanone maleate

References

1. Varga C, et al. Eur J Pharmacol. 2005 Oct 17;522(1-3):130-8.

2. Venable JD, et al. J Med Chem. 2005 Dec 29;48(26):8289-98.

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