JNJ 10191584 maleate

Chemical Structure : JNJ 10191584 maleate

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货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	394.81
分子式	C17H19ClN4O5
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(5-chloro-1H-benzo[d]imidazol-2-yl)(4-methylpiperazin-1-yl)methanone maleate

参考文献

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.