2. Metabolic Enzyme/Protease Anti-infection
  3. Acetyl-CoA synthetase Parasite
  4. MMV693183

MMV693183 是一种口服有效的恶性疟原虫乙酰辅酶 A 合成酶 (AcAS) 抑制剂，对恶性疟原虫的 IC50 为 300 nM。MMV693183 对包括 Artemisinin (HY-B0094) 抗性株在内的疟原虫临床分离株均具有强效抑制活性。MMV693183 可在体内代谢为活性抗代谢物 CoA-MMV693183，通过结合并抑制乙酰辅酶 A 合成酶的功能，降低乙酰辅酶 A 和 4-磷酸泛酸水平，从而发挥杀灭无性血液期寄生虫和阻断向按蚊传播的作用。在人源化小鼠模型中，MMV693183 显示出良好的体内疗效、类药物特性，对人细胞无显著细胞毒性或脱靶活性。MMV693183 可作为杀寄生虫剂及代谢干扰剂，而被广泛应用于疟疾相关研究。

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MMV693183

MMV693183 Chemical Structure

CAS No. : 2446681-27-0

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MMV693183 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

MMV693183 is an orally potent inhibitor of Plasmodium falciparum acetyl-CoA synthetase (AcAS), with an IC50 of 300 nM against Plasmodium falciparum. MMV693183 exhibits potent inhibitory activity against clinical isolates of malaria parasites, including Artemisinin (HY-B0094)-resistant strains. MMV693183 is metabolized in vivo into the active antimetabolite CoA-MMV693183, which exerts effects of killing asexual blood-stage parasites and blocking transmission to Anopheles mosquitoes by binding to and inhibiting the function of acetyl-CoA synthetase, thereby reducing the levels of acetyl-CoA and 4'-phosphopantetheine. In humanized mouse models, MMV693183 shows favorable in vivo efficacy, drug-like properties, and no significant cytotoxicity or off-target activity against human cells. MMV693183 is widely used in malaria-related research as a parasiticide and metabolic disruptor[1].

体外研究
(In Vitro)

MMV693183 可强效抑制恶性疟原虫 (Plasmodium falciparum) 株的体外无性血液期生长，IC50 为 2.1-2.8 nM；同时可抑制恶性疟原虫和间日疟原虫 (P. vivax) 临床分离株的体外生长/裂殖体成熟，活性达低纳摩尔水平[1]。
MMV693183 可抑制恶性疟原虫 NF54-HGL 配子体的活力，72 h 时的 IC50=17.8-38.8 nM；MMV693183 还强效抑制雌配子体活化 (IC50=12 nM)，而对雄配子形成的活性较弱 (IC50=1 µM)[1]。
MMV693183 (1.5 nM, 500 nM; 72 h) 可使恶性疟原虫 AcAS 条件性敲低寄生虫在 AcAS 敲低条件下表现出 5 倍的超敏性[1]。
MMV693183 (10 µM) 在人肝细胞或 HepG2 细胞中无体外细胞毒性，且在 10 µM 浓度下对人受体、酶或通道无显著脱靶活性[1]。

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

MMV693183 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: Human hepatocytes or HepG2 cells
Concentration: 10 µM
Incubation Time: 72 h
Result: Exhibited no in vitro cytotoxicity in human hepatocytes or HepG2 cells.
药代动力学
(Parmacokinetics)
Species Dose Route CLtotal T1/2 Bioavailability
Mice[1] 3 mg/kg i.v. 13.4 mL/min/kg 1.2 h /
Rat[1] 3 mg/kg i.v. 21.1 mL/min/kg 3.1 h /
Dog[1] 1 mg/kg i.v. 11.5 mL/min/kg 4.2 h /
Rat[1] 30 mg/kg p.o. / / 121 %
Dog[1] 2 mg/kg p.o. / / 64 %
体内研究
(In Vivo)

MMV693183 (50 mg/kg；口服；单剂量) 可在 3 天内将人源化 NSG 小鼠体内的恶性疟原虫 (P. falciparum) 引起的疟原虫血症降至检测水平以下[1]。
MMV693183 可在 4-6 天内将人源化 NSG 小鼠体内的恶性疟原虫 (P. falciparum) 血症清除至检测不到的水平，其模拟 MIC 为 3.2 ng/mL，MPC90 为 38.4 ng/mL[1]。
MMV693183 (10-50 mg/kg；每日给药；共 4 天) 不会在植入 G6PD-A 缺陷型人红细胞的 NSG 小鼠中引发溶血毒性[1]。
MMV693183 (10-1000 mg/kg；口服；每日；3-8 天) 在 Wistar Han 大鼠中表现出良好的耐受性，当剂量高达 1000 mg/kg、给药时长 3 天时无明显毒性；在 30 mg/kg/天的剂量下，其暴露安全边际相较于预测的人类有效暴露量超过 30 倍[1]。

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

Animal Model: NSG (female, humanized with G6PD-A-deficient human erythrocytes to achieve >60% human erythrocytes)[1]
Dosage: 10 mg/kg; 25 mg/kg; 50 mg/kg
Administration: daily; 4 days
Result: Showed no signs of hemolytic toxicity; did not induce hemolysis of G6PD-A-deficient human erythrocytes.
分子量

362.34

Formula

C16H21F3N2O4
CAS 号
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

MMV693183 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

MMV6931832446681-27-0MMV 693183MMV-693183Acetyl-CoA synthetaseParasiteAcsAnopheles mosquitoesartemisinin-resistant P. falciparum field isolateshuman hepatocytesNSG miceacetyl-CoA synthetasehumanized mouse modelHepG2 cellsWistar Han ratsPlasmodium vivaxPlasmodium falciparumInhibitorinhibitorinhibit

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