869497-75-6
Chemical Structure
JNJ10191584 maleate
Synonym(s): VUF6002 maleate
- CAS No.: 869497-75-6
- Formula:C17H19ClN4O5
- Molecular Weight:394.81
IUPAC Name: (5-chloro-1H-benzo[d]imidazol-2-yl)(4-methylpiperazin-1-yl)methanone maleate
InChIKey: KOTJFAYEELTYCZ-BTJKTKAUSA-N
SMILES: OC(/C=C\C(O)=O)=O.O=C(N1CCN(CC1)C)C2=NC3=CC(Cl)=CC=C3N2
Biological Activity: JNJ10191584 (VUF6002) maleate (compound 40) is an orally active and selective histamine H4 receptor antagonist with a Ki value of 26 nM. JNJ10191584 maleate shows 540-fold selectivity to H4 receptor over the H3 receptor with a Ki value of 14.1 μM. JNJ10191584 maleate inhibits chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively[1][2].
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JNJ10191584 maleate | JNJ10191584 (VUF6002) maleate (compound 40) is an orally active and selective histamine H4 receptor antagonist with a Ki value of 26 nM. JNJ10191584 maleate shows 540-fold selectivity to H4 receptor over the H3 receptor with a Ki value of 14.1 μM. JNJ10191584 maleate inhibits chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively. | |||||||||||||||||||||
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References
- [1]. Venable JD, et al. Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists. J Med Chem. 2005 Dec 29;48(26):8289-98. [Content Brief]
- [2]. Sanna MD, et al. Histamine H4 receptor stimulation in the locus coeruleus attenuates neuropathic pain by promoting the coeruleospinal noradrenergic inhibitory pathway. Eur J Pharmacol. 2020 Feb 5;868:172859. [Content Brief]
