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Eflornithine

Catalog No. T40811 CAS 70052-12-9

Synonyms: RMI71782, α-difluoromethylornithine, DFMO, MDL71782

Eflornithine is an irreversible inhibitor that specifically targets the enzyme ornithine decarboxylase. It serves as a therapeutic medication for two conditions: the treatment of African trypanosomiasis and the management of excessive facial hair growth in women.

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Eflornithine, CAS 70052-12-9

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Biological Description

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Description

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].

Synonyms	RMI71782, α-difluoromethylornithine, DFMO, MDL71782
Molecular Weight	182.17
Formula	C6H12F2N2O2
CAS No.	70052-12-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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

Citations

1. Mastrodomenico V, LoMascolo N J, Firpo M R, et al.Persistent Coxsackievirus B3 Infection in Pancreatic Ductal Cells In Vitro Downregulates Cellular Polyamine Metabolism.Msphere.2023: e00036-23.

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Eflornithine 70052-12-9 RMI-71782 RMI71782 α-difluoromethylornithine DFMO MDL-71782 a-difluoromethylornithine RMI 71782 MDL71782 alpha-difluoromethylornithine MDL 71782 inhibitor inhibit

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