2. Metabolic Enzyme/Protease Anti-infection GPCR/G Protein Neuronal Signaling Immunology/Inflammation Membrane Transporter/Ion Channel
  3. Drug Metabolite Parasite Histamine Receptor Potassium Channel
  4. Desmethylastemizole

Desmethylastemizole  (Synonyms: O-Demethylastemizole)

目录号: HY-W516880
产品使用指南 技术支持

Desmethylastemizole (O-Demethylastemizole) 是一种 Astemizole (HY-12532) 代谢物，是一种 β-血红素 (βH) 抑制剂。Desmethylastemizole 具有抗恶性疟原虫活性，对 Pf3D7、PfDd2 和 PfItG 株 的 IC50 分别为 0.12 μM、0.11 μM 和 0.06 μM。Desmethylastemizole 也是一种组胺 H1 受体 (Histamine H1 receptor) 拮抗剂。Desmethylastemizole 能显著阻断 hERG K+ 通道，并抑制组蛋白-赖氨酸 N-甲基转移酶 EZH2 的活性。Desmethylastemizole 可用于长 QT 综合征和疟疾研究。

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Desmethylastemizole

Desmethylastemizole Chemical Structure

CAS No. : 73736-50-2

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1 mg ￥5040
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Desmethylastemizole 相关抗体

Top Publications Citing Use of Products

查看 Parasite 亚型特异性产品:

查看所有亚型
Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

查看 Histamine Receptor 亚型特异性产品:

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H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Desmethylastemizole (O-Demethylastemizole) , a metabolite of Astemizole (HY-12532), is a β-hematin (βH) inhibitor. Desmethylastemizole has an antiplasmodium activity against P. falciparum with IC50 of 0.12, 0.11 and 0.06  μM for Pf3D7, PfDd2, and PfItG strains, respectively. Desmethylastemizole is also a Histamine H1 receptor antagonist. Desmethylastemizole significantly blocks hERG K+ channels and also inhibits histone-lysine N-methyltransferase EZH2 activity. Desmethylastemizole can be used for long QT syndrome and malaria research[1][2][3].

IC50 & Target[1][3]

H1 Receptor

 

Plasmodium falciparum sporozoites

 

分子量

444.54

Formula

C27H29FN4O
CAS 号
性状

固体

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

纯度 & 产品资料
参考文献

Desmethylastemizole 相关分类

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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.

Keywords:

Desmethylastemizole73736-50-2O-DemethylastemizoleDrug MetaboliteParasiteHistamine ReceptorPotassium ChannelKcsAAstemizoleβ-hematinβHP. falciparumHistamine H1 receptorhERG K+ channelsLong QT syndromeMalariaInhibitorinhibitorinhibit

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