依氟鸟氨酸盐酸盐一水合物 原粉 99%主打

生物活性Eflornithine(Difluoromethylornithine,DFMO,MDL-71782,RMI-71782,α-difluoromethylornithine)hydrochloridehydrate通过对鸟氨酸脱羧酶的不可逆抑制作用，抑制多胺生物合成。它是一种化疗保护剂，可阻止血管生成。其生物半衰期为8小时。靶点TargetValueOrndecarboxylase体外研究用α-difluoromethyl-Orn处理BY2细胞，抑制其过氧化氢的产生，但并没有发生程序性细胞死亡。体内研究EflornithineistheonlynewmoleculeregisteredforthetreatmentofhumanAfricantrypanosomiasisoverthelast50years.Itisthedrugusedmainlyasaback-upformelarsoprolrefractoryTrypanosomabruceigambiensecases.Insubjectswithexcessive,unwantedfacialhair,eflornithine15%creamissuperiortoplaceboinreducinghairgrowth.After24weeks'treatment,58%ofeflornithineand34%ofplacebosubjectshaveatleastsomeimprovementinfacialhirsutism.Thehairgrowthinhibitoryactivityofeflornithineissignificantlyenhancedwhentheeflornithinecreamisappliedontoamouseskinareapretreatedwithmicroneedles.TreatmentofcoarctationhypertensiveratswitheflornithineresultsinanormalizationofthecontractileintensitytoKCIandnorepinephrineandrelaxationstoacetylcholineby14daysofhypertension.