Fexinidazole (HOE 239) (HOE 239) 是一种具有口服活性的强效硝基咪唑类抗锥虫药物。
Cas No. | 59729-37-2 |
别名 | 非昔硝唑; HOE 239 |
Canonical SMILES | O=[N+](C1=CN=C(COC2=CC=C(SC)C=C2)N1C)[O-] |
分子式 | C12H13N3O3S |
分子量 | 279.31 |
溶解度 | DMSO : 50 mg/mL (179.01 mM);Water :< 0.1 mg/mL (insoluble) |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | Fexinidazole is a 5-nitroimidazole drug currently in clinical development for the treatment of human sleeping sickness (human African trypanosomiasis [HAT]), caused by infection with species of the protozoan parasite Trypanosoma brucei. Target: Antiparasiticin vivo: Fexinidazole shows dose-related efficacy in the T. b. rhodesiense (STIB900) acute mouse model at intraperitoneal (i.p.) doses of 20 to 50 mg/kg/day and oral (per os [p.o.]) doses of 25 to 100 mg/kg/day given on four consecutive days, with 100 mg/kg/day p.o. being 100% curative. Fexinidazole is shown to be effective in the GVR35 mouse model, which mimics the advanced and fatal stage of the disease, when parasites have disseminated into the brain. [1] [1]. Kaiser M, 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. |