1. Anti-infection
  2. Parasite
  3. Antimalarial agent 52

Antimalarial agent 52 是一种口服有效的合成疟色素 (β-hematin) 抑制剂,其 IC50 为 6.6 μM。Antimalarial agent 52 在体外对恶性疟原虫 Pf3D7PfDd2 菌株和诺氏疟原虫 P. knowlesi 表现出抗疟活性,其 IC50 分别为 6.1、6.4 和 3.3 nM。Antimalarial agent 52 对多重耐药菌株仍然保持高效,且在伯氏疟原虫 (P. berghei) 小鼠模型中有显著疗效。

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Antimalarial agent 52

Antimalarial agent 52 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Antimalarial agent 52 is an orally active formation of synthetic hemozoin (β-hematin) inhibitor with an IC50 of 6.6 μM. Antimalarial agent 52 exhibits in vitro antiplasmodial activity against P. falciparum Pf3D7, PfDd2 strains and P. knowlesi with IC50s of 6.1, 6.4 and 3.3 nM. Antimalarial agent 52 remain highly effective against multidrug-resistant strains and demonstrates curative activity in the P. berghei mouse model[1].

体外研究
(In Vitro)

Antimalarial agent 52 (Compound 7d) (48 h) 对疟疾患者分离株和耐药突变株表现出抗疟原虫活性,IC50 分别为 4-16 nM 和 8-15 nM[1]
Antimalarial agent 52 不被人肝微粒体代谢,具有较高的血浆稳定性,并显示出改善的心脏安全性[1]

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

体内研究
(In Vivo)

Antimalarial agent 52 (Compound 7d) (3-50 mg/kg,口服,感染后 4、24、48、72 小时,共 4 次) 在 30 和 50 mg/kg 剂量下在 P. berghei 小鼠模型中达到 100% 的治愈率[1]

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

Animal Model: P. berghei infection model established in female NMRI mice[1]
Dosage: 3, 10, 30 and 50 mg/kg
Administration: Oral administration (p.o.), 4, 24, 48, 72 hours after infection for 4 doses
Result: Showed significant dose-dependent antimalarial activity.
分子量

559.75

Formula

C24H17BrClF5N2O

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.

纯度 & 产品资料
参考文献

Antimalarial agent 52 相关分类

  • 摩尔计算器

  • 稀释计算器

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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Help & FAQs
  • 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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Antimalarial agent 52
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HY-178147
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