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[1][2].

Product Specifications

CAS Number

[869497-75-6]

Product Name Alternative

VUF6002 (maleate)

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Histamine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/jnj10191584-maleate.html

Solubility

10 mM in DMSO

Smiles

OC(/C=C\C(O)=O)=O.O=C(N1CCN(CC1)C)C2=NC3=CC(Cl)=CC=C3N2

Molecular Formula

C17H19ClN4O5

Molecular Weight

394.81

Precautions

H302, H315, H319, H335

References & Citations

[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.|[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.