JNJ10191584,869497-75-6

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JNJ10191584 maleate

CAS No. : 869497-75-6

MCE 国际站：JNJ10191584 maleate

产品活性：JNJ10191584 (VUF6002) maleate (compound 40) 是具有口服活性的、选择性 histamine H₄ 受体 拮抗剂，K_i 值为 26 nM。JNJ10191584 maleate 对 H₄ 受体的选择性是 H₃ 受体的 540 倍，对 H₃ 受体的 K_i 值为 14.1 μM。JNJ10191584 maleate 抑制嗜酸性粒细胞和肥大细胞的趋化作用，IC₅₀ 值分别为 530 nM 和 138 nM。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Immunology/Inflammation

作用靶点：Histamine Receptor

In Vitro: 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.

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.
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.

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