| Name | JNJ 10191584 maleate,1-[(5-Chloro-1H-benzimidazol-2-yl)carbonyl]-4-methylpiperazinemaleate |
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| Synonyms | vuf 6002 |
| 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]. |
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| Related Catalog | |
| 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]. |
| 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 |
| Symbol |
GHS07 |
|---|---|
| Signal Word | Warning |
| Hazard Statements | H302-H315-H319-H335 |
| Precautionary Statements | P261-P305 + P351 + P338 |
| RIDADR | NONH for all modes of transport |