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.
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快速发货 顺丰冷链运输,1-2 天到达
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免费溶解
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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]. |
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 << |
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 |
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 |