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非昔硝唑 /Fexinidazole {[allProObj[0].p_purity_real_show]}

货号:A322155 同义名: HOE 239;Fexinidazole Winthrop

Fexinidazole is a 5-nitroimidazole drug for the treatment of human sleeping sickness (human African trypanosomiasis [HAT]), caused by infection with species of the protozoan parasite Trypanosoma brucei.

Fexinidazole 化学结构 CAS号:59729-37-2
Fexinidazole 化学结构
CAS号:59729-37-2
Fexinidazole 3D分子结构
CAS号:59729-37-2
Fexinidazole 化学结构 CAS号:59729-37-2
Fexinidazole 3D分子结构 CAS号:59729-37-2
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Fexinidazole 纯度/质量文件 产品仅供科研

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Fexinidazole 生物活性

靶点
  • DNA synthesis

描述 Human African Trypanosomiasis (HAT), or sleeping sickness, is a life-threatening, neglected tropical disease (NTD). The etiological agent of HAT is the kinetoplastid protozoan parasite Trypanosoma brucei (T. b.). Two subspecies of this parasite are pathogenic for humans: T. b. gambiense (g-HAT) responsible for the chronic form of the disease occurring in western and central Africa, and T. b. rhodesiense (r-HAT) responsible for a more acute form occurring in eastern and southern Africa. Fexinidazole, a 5-nitroimidazole derivative DNA synthesis inhibitor, is the only, all-oral treatment for HAT and is indicated for use by adults and children (aged ≥ 6 years and weighing ≥ 20 kg) for both g-HAT stages[3]. This molecule and its metabolites (sulfoxide and sulfone) have shown trypanocidal activity in vitro in the 0.7-to-3.3 μM (0.2-to-0.9 μg/ml) range against all parasite strains tested. In vivo, fexinidazole is orally effective in curing both acute and chronic diseases in the mouse at doses of 100 mg/kg of body weight/day for 4 days and 200 mg/kg/day for 5 days, respectively[4].

Fexinidazole 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02571062 Trypanosomiasis, African Phase 1 Completed - France ... 展开 >> Biotrial Rennes, France 收起 <<
NCT02498782 Chagas Disease ... 展开 >> Trypanosomiasis, South American South American Trypanosomiasis Disease, Chagas 收起 << Phase 2 Unknown February 2016 Bolivia ... 展开 >> Plataforma Atención Integral de Pacientes con Enfermedad de Chagas Recruiting Cochabamba, Bolivia Contact: Faustino Torrico, MD    59177411905    foxtorrico@yahoo.com    Contact: Cristina Alonso, MD    59172211312    calonso@dndi.org    Principal Investigator: Faustino Torrico, MD          Plataforma de Atención Integral de Pacientes con Enfermedad de Chagas Recruiting Tarija, Bolivia Contact: Lourdes O Daza, MD    5916672252    lourdesortizd@yahoo.es    Contact: Erika Ribeiro, Pharm D    59175969924    ecorreia@dndi.org    Principal Investigator: Lourdes O Daza, MD 收起 <<
NCT01483170 Trypanosomiasis, African Phase 1 Terminated(poor tolerability a... 展开 >>t highest dose) 收起 << - France ... 展开 >> SGS Life Sciences Paris, France, 75015 收起 <<

Fexinidazole 参考文献

[1]Kaiser M, Bray MA, et al. Antitrypanosomal activity of fexinidazole, a new oral nitroimidazole drug candidate for treatment of sleeping sickness. Antimicrob Agents Chemother. 2011 Dec;55(12):5602-8.

[2]Torreele E, Bourdin Trunz B, et al. Fexinidazole--a new oral nitroimidazole drug candidate entering clinical development for the treatment of sleeping sickness. PLoS Negl Trop Dis. 2010 Dec 21;4(12):e923.

[3]Innovative Partnerships for the Elimination of Human African Trypanosomiasis and the Development of Fexinidazole

[4]Antitrypanosomal Activity of Fexinidazole, a New Oral Nitroimidazole Drug Candidate for Treatment of Sleeping Sickness

Fexinidazole 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.58mL

0.72mL

0.36mL

17.90mL

3.58mL

1.79mL

35.80mL

7.16mL

3.58mL

Fexinidazole 技术信息

CAS号59729-37-2
分子式C12H13N3O3S
分子量 279.315
别名 HOE 239;Fexinidazole Winthrop
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Room Temperature

溶解度

DMSO: 50 mg/mL(179.01 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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