73903-17-0
Chemical Structure
JNJ10191584
Synonym(s): VUF6002
- CAS No.: 73903-17-0
- Formula:C13H15ClN4O
- Molecular Weight:278.74
IUPAC Name: (5-chloro-1H-benzo[d]imidazol-2-yl)(4-methylpiperazin-1-yl)methanone
InChIKey: MOIWSUQWIOVGRH-UHFFFAOYSA-N
SMILES: O=C(N1CCN(CC1)C)C2=NC3=CC(Cl)=CC=C3N2
Biological Activity: JNJ10191584 (VUF6002) is an orally active and selective histamine H4 receptor antagonist with a Ki value of 26 nM. JNJ10191584 shows 540-fold selectivity to H4 receptor over H3 receptor with a Ki value of 14.1 μM. JNJ10191584 inhibits chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively[1][2].
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JNJ10191584 | 99.90% | JNJ10191584 (VUF6002) is an orally active and selective histamine H4 receptor antagonist with a Ki value of 26 nM. JNJ10191584 shows 540-fold selectivity to H4 receptor over H3 receptor with a Ki value of 14.1 μM. JNJ10191584 inhibits chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively. | ||||||||||||||||||||
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- [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]
Keywords
