JNJ 10191584 maleate

Pricing Availability   Qty
说明: Selective H4 antagonist; orally active
别名: VUF 6002
化学名: 1-[(5-Chloro-1H-benzimidazol-2-yl)carbonyl]-4-methylpiperazine maleate
纯度: ≥99% (HPLC)
说明书
引用文献 (3)
评论
文献 (1)

生物活性 for JNJ 10191584 maleate

JNJ 10191584 maleate is a highly selective histamine H4 receptor silent antagonist; binds with high affinity to the human H4 receptor (Ki = 26 nM). > 540-fold selective over the H3 receptor (Ki = 14.1 μM). Inhibits mast cell and eosinophil chemotaxis in vitro with IC50 values of 138 and 530 nM respectively. Orally active in vivo.

化合物库 for JNJ 10191584 maleate

JNJ 10191584 maleate is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。

技术数据 for JNJ 10191584 maleate

分子量 394.81
公式 C13H15ClN4O.C4H4O4
储存 Desiccate at RT
纯度 ≥99% (HPLC)
CAS Number 869497-75-6
PubChem ID 11718163
InChI Key KOTJFAYEELTYCZ-BTJKTKAUSA-N
Smiles O=C(O)/C=C\C(O)=O.ClC(C=C3)=CC2=C3N=C(N2)C(N1CCN(C)CC1)=O

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for JNJ 10191584 maleate

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 19.74 50

制备储备液 for JNJ 10191584 maleate

以下数据基于产品分子量 394.81。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
0.5 mM 5.07 mL 25.33 mL 50.66 mL
2.5 mM 1.01 mL 5.07 mL 10.13 mL
5 mM 0.51 mL 2.53 mL 5.07 mL
25 mM 0.1 mL 0.51 mL 1.01 mL

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产品说明书 for JNJ 10191584 maleate

参考文献 for JNJ 10191584 maleate

参考文献是支持产品生物活性的出版物。

Terzioglu et al (2004) Synthesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H4 receptor antagonists. Bioorg.Med.Chem.Lett. 14 5251 PMID: 15454206

Venable et al (2005) Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine H4 antagonists. J.Med.Chem. 48 8289 PMID: 16366610

Varga et al (2005) Inhibitory effects of histamine H4 receptor antagonists on experimental colitis in the rat. Eur.J.Pharmacol. 522 130 PMID: 16213481


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关键词: JNJ 10191584 maleate, JNJ 10191584 maleate supplier, Selective, H4, receptor, antagonists, orally, active, Receptors, Histamine, histaminergic, JNJ10191584, maleate, VUF6002, silent, antagonist, VUF, 6002, 2441, Tocris Bioscience

3 篇 JNJ 10191584 maleate 的引用文献

引用文献是使用了 Tocris 产品的出版物。 JNJ 10191584 maleate 的部分引用包括:

Desmadryl et al (2012) Histamine H4 receptor antagonists as potent modulators of mammalian vestibular primary neuron excitability. Br J Pharmacol 167 905 PMID: 22624822

Connelly et al (2009) The histamine H4 receptor is functionally expressed on neurons in the mammalian CNS. Br J Pharmacol 157 55 PMID: 19413571

Tanaka et al (2016) Histamine H3 receptor antagonist OUP-186 attenuates the proliferation of cultured human breast cancer cell lines Biochemical and Biophysical Research Communication 480 479 PMID: 27773822


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Histamine Receptors Scientific Review

Histamine Receptors Scientific Review

Written by Iwan de Esch and Rob Leurs, this review provides a synopsis of the different histamine receptor subtypes and the ligands that act upon them; compounds available from Tocris are listed.