| 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]. |
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| Related Catalog | |
| 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]. |
| Molecular Formula | C13H15ClN4O |
|---|---|
| Molecular Weight | 278.73700 |
| Exact Mass | 278.09300 |
| PSA | 52.23000 |
| LogP | 1.47970 |