73903-17-0

73903-17-0 structure

Name: (6-CHLORO-1H-BENZOIMIDAZOL-2-YL)-(4-METHYL-PIPERAZIN-1-YL)-METHANONE
Chemical Name: 1-(5-chloro-1(3)H-benzoimidazole-2-carbonyl)-4-methyl-piperazine
CAS Number: 73903-17-0
Molecular Formula: C₁₃H₁₅ClN₄O
Molecular Weight: 278.73700
Catalog: Signaling Pathways GPCR/G Protein Histamine Receptor
Create Date: 2018-05-21 23:56:50
Modify Date: 2024-04-05 17:11:17
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].

Name	1-(5-chloro-1(3)H-benzoimidazole-2-carbonyl)-4-methyl-piperazine
Synonyms	jnj 10191584

Description	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].
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 shows binding affinity of 26 nM and 14.1 μM to H4 and H3 receptor, respectively[1]. JNJ10191584 (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 (10 μg/μL; intra locus coeruleus (LC) administration; once) abolishs VUF-induced anti-allodynic effect in spared nerve injury (SNI) mice[1]. JNJ10191584 (10 μg/μL; intra LC administration; once) prevents the anti-allodynic effect of VUF 8430 in SNI mice[1]. JNJ10191584 (6 μg/mouse; intrathecal administration; pretreat once) prevents VUF 8430-induced anti-allodynic effect in SNI mice[1].