VUF6002

Names

[ Name ]:
VUF6002

[Synonym ]:
vuf 6002

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> Histamine Receptor

[Target]

Human H4 Receptor:26 nM (Ki)

human H3 receptor:14.1 μM (Ki)

[In Vitro]

JNJ10191584 maleate shows binding affinity of 26 nM and 14.1 μM to H4 and H3 receptor, respectively[1]. JNJ10191584 maleate (3 h) shows inhibitory effects to chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively[1].

[In Vivo]

JNJ10191584 maleate (10 μg/μL; intra locus coeruleus (LC) administration; once) abolishs VUF-induced anti-allodynic effect in spared nerve injury (SNI) mice[1]. JNJ10191584 maleate (10 μg/μL; intra LC administration; once) prevents the anti-allodynic effect of VUF 8430 in SNI mice[1]. JNJ10191584 maleate (6 μg/mouse; intrathecal administration; pretreat once) prevents VUF 8430-induced anti-allodynic effect in SNI mice[1].

Chemical & Physical Properties

[ Boiling Point ]:
461ºC at 760 mmHg

[ Molecular Formula ]:
C₁₇H₁₉ClN₄O₅

[ Molecular Weight ]:
394.81000

[ Flash Point ]:
232.6ºC

[ Exact Mass ]:
394.10400

[ PSA ]:
126.83000

[ LogP ]:
1.19150

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302-H315-H319-H335

[ Precautionary Statements ]:
P261-P305 + P351 + P338

[ RIDADR ]:
NONH for all modes of transport