产品说明书

Fexinidazole

Print
Chemical Structure| 59729-37-2 同义名 : HOE 239;Fexinidazole Winthrop
CAS号 : 59729-37-2
货号 : A322155
分子式 : C12H13N3O3S
纯度 : 98%
分子量 : 279.315
MDL号 : MFCD00866607
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
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：
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].
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 <<
实验方案
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
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