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JNJ10191584 maleate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
JNJ10191584 maleate图片
CAS NO:869497-75-6
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
VUF6002 maleate
产品介绍
JNJ10191584 (VUF6002) maleate (compound 40) 是具有口服活性的、选择性 histamineH4受体拮抗剂,Ki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Ki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。
生物活性

JNJ10191584 (VUF6002) maleate (compound 40) is an orally active and selective histamineH4receptorantagonist with aKivalue of 26 nM. JNJ10191584 maleate shows 540-fold selectivity toH4receptorover theH3receptorwith aKivalue of 14.1 μM. JNJ10191584 maleate inhibits chemotaxis of eosinophils and mast cells withIC50values of 530 nM and 138 nM, respectively[1][2].

IC50& Target

Human H4Receptor

26 nM (Ki)

human H3receptor

14.1 μM (Ki)

体外研究
(In Vitro)

JNJ10191584 maleate shows binding affinity of 26 nM and 14.1 μM to H4and H3receptor, respectively[1].
JNJ10191584 maleate (3 h) shows inhibitory effects to chemotaxis of eosinophils and mast cells with IC50values of 530 nM and 138 nM, respectively[1].

体内研究
(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].

分子量

394.81

Formula

C17H19ClN4O5

CAS 号

869497-75-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.