产品
编 号：F488840
分子式：C17H19ClN4O5
分子量：394.81
分子式：C17H19ClN4O5
分子量：394.81
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CAS No: 869497-75-6
产品详情
生物活性：
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.
体内研究：
JNJ10191584 maleate (10 μg/μL; intra locus coeruleus (LC) administration; once) abolishs VUF-induced anti-allodynic effect in spared nerve injury (SNI) mice.JNJ10191584 maleate (10 μg/μL; intra LC administration; once) prevents the anti-allodynic effect of VUF 8430 in SNI mice.JNJ10191584 maleate (6 μg/mouse; intrathecal administration; pretreat once) prevents VUF 8430-induced anti-allodynic effect in SNI mice.
体外研究：
JNJ10191584 maleate shows binding affinity of 26 nM and 14.1 μM to H4 and H3 receptor, respectively.JNJ10191584 maleate (3 h) shows inhibitory effects to chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively.
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.
体内研究：
JNJ10191584 maleate (10 μg/μL; intra locus coeruleus (LC) administration; once) abolishs VUF-induced anti-allodynic effect in spared nerve injury (SNI) mice.JNJ10191584 maleate (10 μg/μL; intra LC administration; once) prevents the anti-allodynic effect of VUF 8430 in SNI mice.JNJ10191584 maleate (6 μg/mouse; intrathecal administration; pretreat once) prevents VUF 8430-induced anti-allodynic effect in SNI mice.
体外研究：
JNJ10191584 maleate shows binding affinity of 26 nM and 14.1 μM to H4 and H3 receptor, respectively.JNJ10191584 maleate (3 h) shows inhibitory effects to chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively.
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