1. Anti-infection Neuronal Signaling Metabolic Enzyme/Protease
  2. Parasite Adenosine Kinase
  3. Antiparasitic agent-30

Antiparasitic agent-30 是一种高效的腺苷激酶 TbrAK 调节剂和抗锥虫剂。Antiparasitic agent-30 对罗德西亚锥虫表现出显著的抑制活性,同时能够增强重组 TbrAK 的活性 (EC50=38 nM,Ka=75 nM-497 nM)。Antiparasitic agent-30 通过消除固有底物抑制作用,过度激活罗德西亚锥虫的 TbrAK 从而发挥药效。Antiparasitic agent-30 可作为研究急性型非洲人类锥虫病 (昏睡病) 的重要工具分子。

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Antiparasitic agent-30

Antiparasitic agent-30 Chemical Structure

CAS No. : 671754-20-4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Antiparasitic agent-30 is a potent adenosine kinase TbrAK modulator and antitrypanosomal agent. Antiparasitic agent-30 exhibits significant inhibitory activity against Trypanosoma brucei rhodesiense, while enhancing the activity of recombinant TbrAK(EC50=38 nM, Ka=75 nM-497 nM). Antiparasitic agent-30 exerts its pharmacological effects by eliminating intrinsic substrate inhibition and hyperactivating TbrAK in Trypanosoma brucei rhodesiense. Antiparasitic agent-30 serves as a valuable tool molecule for studying acute African human trypanosomiasis (sleeping sickness).

IC50 & Target

Trypanosoma

1 μM (IC50)

体外研究
(In Vitro)

Antiparasitic agent-30 (Compound 1) 可强效抑制 T. b. rhodesiense 寄生虫的活力,其 IC50 为 1.0 μM[1]
Antiparasitic agent-30 (1-750 μM; 10 min) 以浓度依赖的方式增强重组 TbrAK 的活性,其 EC50 为 38.9 μM,在 50 μM 时活性提升 2.5 倍[1]
Antiparasitic agent-30 在放射分析实验中可增强重组 TbrAK 的活性,其高效能 EC50 为 38 nM[1]
Antiparasitic agent-30 (150 μM) 可与重组 TbrAK (7 μM) 的两个不同位点结合,对主要结合位点表现出高亲和力 (Kd=75 nM)[1]
Antiparasitic agent-30 对 TbAK 沉默的 T. b. brucei 寄生虫的效力降低,其 IC50 从 131 nM 升高至 271 nM,证实其活性依赖于腺苷激酶的表达[1]

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

分子量

321.37

Formula

C19H19N3O2

CAS 号
性状

固体

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

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Antiparasitic agent-30
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HY-179690
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