Eflornithine (DFMO) 是酶鸟氨酸脱羧酶的特

Eflornithine  (Synonyms: 依氟乌氨酸; DFMO; MDL71782; RMI71782; α-difluoromethylornithine)

Eflornithine (DFMO) 是酶鸟氨酸脱羧酶的特异性不可逆抑制剂。Eflornithine 可用于研究非洲锥虫病和女性面部毛发过度生长。

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生物活性    
Eflornithine is a specific, irreversible inhibitor of the enzyme ornithine decarboxylase. Eflornithine is a medication for the treatment of African trypanosomiasis and excessive facial hair growth in women.

IC50 & Target    
Trypanosoma

体内研究
(In Vivo)    
Eflornithine is the only new molecule registered for the treatment of human African trypanosomiasis over the last 50 years. It is the drug used mainly as a back-up for melarsoprol refractory Trypanosoma brucei gambiense cases[1]. In subjects with excessive, unwanted facial hair, eflornithine 15% cream is superior to placebo in reducing hair growth. After 24 weeks' treatment, 58% of eflornithine and 34% of placebo subjects have at least some improvement in facial hirsutism[2]. The hair growth inhibitory activity of eflornithine is significantly enhanced when the eflornithine cream is applied onto a mouse skin area pretreated with microneedles[3]. Treatment of coarctation hypertensive rats with eflornithine results in a normalization of the contractile intensity to KCI and norepinephrine and relaxations to acetylcholine by 14 days of hypertension[4].

分子量    
182.17

Formula    
C6H12F2N2O2

CAS 号    
70052-12-9

中文名称    
依氟乌氨酸

运输条件    
Room temperature in continental US; may vary elsewhere.

储存方式    
Please store the product under the recommended conditions in the Certificate of Analysis.
 

参考文献

[1]. Burri C, et al. Eflornithine for the treatment of human African trypanosomiasis. Parasitol Res. 2003 Jun;90 Supp 1:S49-52.  [Content Brief] [2]. Balfour JA, et al. Topical eflornithine. Am J Clin Dermatol. 2001;2(3):197-201; discussion 202.  [Content Brief] [3]. Kumar A, et al. A method to improve the efficacy of topical eflornithine hydrochloride cream. Drug Deliv. 2016 Jun;23(5):1495-501.  [Content Brief] [4]. Lipke DW, et al. Eflornithine alters changes in vascular responsiveness associated with coarctation hypertension. Clin Exp Hypertens. 1997 Apr;19(3):297-312.  [Content Brief]

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