2. Anti-infection Metabolic Enzyme/Protease
  3. Parasite Aminopeptidase
  4. Antimalarial agent 55

Antimalarial agent 55 是一种口服有效的恶性疟原虫 PfA-M1 和 PfA-M17 氨肽酶抑制剂，其 Ki 分别为 27 和 81 nM。Antimalarial agent 55 对间日疟和伯氏疟原虫同源酶均表现出纳摩尔级的强效活性，其对于 Pv-M1、Pb-M1、Pv-M17 和 Pb-M17 的 Ki 值分别为 2、4、190 和 18 nM。Antimalarial agent 55 具有显著的抗疟原虫活性，且具备交叉物种抑制能力和不受现有耐药机制影响的广谱活性。Antimalarial agent 55 可用于疟疾的研究。

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Antimalarial agent 55

Antimalarial agent 55 Chemical Structure

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Antimalarial agent 55 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Antimalarial agent 55 is an orally potent inhibitor of PfA-M1 and PfA-M17 aminopeptidases from Plasmodium falciparum, with Ki values of 27 nM and 81 nM, respectively. Antimalarial agent 55 exhibits potent nanomolar activity against homologous enzymes from Plasmodium vivax and Plasmodium berghei, with Ki values of 2 nM, 4 nM, 190 nM and 18 nM for Pv-M1, Pb-M1, Pv-M17 and Pb-M17, respectively. Antimalarial agent 55 possesses significant antiplasmodial activity, as well as cross-species inhibitory capacity and broad-spectrum activity that is unaffected by existing drug resistance mechanisms. Antimalarial agent 55 can be used in malaria research[1].

体外研究
(In Vitro)

Antimalarial agent 55 (Compound 3k) (72 h) 对恶性疟原虫株 Pf3D7 具有体外杀伤活性，其 EC50 为 31 nM；对不同耐药机制的恶性疟原虫临床分离株同样有着强效的活性。

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

Antimalarial agent 55 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Clearance (CL) T1/2 Vss B/P Bioavailability Cmax Tmax
Mice[1] 1 mg/kg i.v. 36.1 mL/min/kg 0.86 h 0.447 L/kg 0.75 / / /
Mice[1] 3 mg/kg p.o. / 11 h / / 61.8 % 2.04 μM 0.25 h
Mice[1] 50 mg/kg p.o. / 7.2 h / / 63.4 % 20 μM 0.25 h
体内研究
(In Vivo)

Antimalarial agent 55 (Compound 3k) (50 mg/kg; p.o.; 4 次给药) 对感染 Plasmodium berghei 的瑞士小鼠，在感染后第 3 天可实现 100% 的抗疟活性[1]。

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

Animal Model: Arc:Arc(Swiss) (female, 6-weeks of age, intraperitoneal infection with 2 × 107 Plasmodium berghei ANKA-infected erythrocytes)[1]
Dosage: 50 mg/kg
Administration: p.o.; at 2 h, day 1, day 2, and day 3 postinfection
Result: Achieved 100% antimalarial activity at 3 days post-infection.\nAchieved 83% antimalarial activity at 4 days post-infection.\nAchieved 63% antimalarial activity at 6 days post-infection.
分子量

315.37

Formula

C17H21N3O3
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 55 相关分类

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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.

Keywords:

Antimalarial agent 55Antimalarial agent55Antimalarial agent-55ParasiteAminopeptidasePlasmodium falciparum M17Plasmodium berghei M17Plasmodium berghei M1Plasmodium aminopeptidasePlasmodium falciparum M1human embryonic kidney cellsPlasmodium vivax M17Plasmodium vivax M1Plasmodium falciparum strainshuman cytochrome P450 isoformsInhibitorinhibitorinhibit

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