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Submit ReviewJNJ 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.
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。
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 19.74 | 50 |
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.
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 |
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
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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