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  2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. JNJ10191584 maleate

JNJ10191584 maleate  (Synonyms: VUF6002 maleate)

目錄號(hào): HY-107558
產(chǎn)品使用指南

JNJ10191584 (VUF6002) maleate (compound 40) 是具有口服活性的、選擇性 histamine H4 受體 拮抗劑，Ki 值為 26 nM。JNJ10191584 maleate 對(duì) H4 受體的選擇性是 H3 受體的 540 倍，對(duì) H3 受體的 Ki 值為 14.1 μM。JNJ10191584 maleate 抑制嗜酸性粒細(xì)胞和肥大細(xì)胞的趨化作用，IC50 值分別為 530 nM 和 138 nM。

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JNJ10191584 maleate Chemical Structure

JNJ10191584 maleate Chemical Structure

CAS No. : 869497-75-6

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JNJ10191584 maleate 的其他形式現(xiàn)貨產(chǎn)品:

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查看 Histamine Receptor 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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[1][2].

IC50 & Target

Human H4 Receptor

26 nM (Ki)

human H3 receptor

14.1 μM (Ki)

體外研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

394.81

Formula

C17H19ClN4O5
CAS 號(hào)
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
純度 & 產(chǎn)品資料
參考文獻(xiàn)

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  • 稀釋計(jì)算器

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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產(chǎn)品名稱：
JNJ10191584 maleate
目錄號(hào)：
HY-107558
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