| Description | Eflornithine hydrochloride hydrate (RMI-71782 hydrochloride hydrate) is a specific, irreversible inhibitor of ornithine decarboxylase. |
| In vitro | When cultured cells are treated with α-difluoromethyl-Orn, an inhibitor of polyamine biosynthesis, production of hydrogen peroxide is suppressed and programmed cell death did not occur[1]. |
| 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[2]. Eflornithine 15% cream is superior to a placebo in reducing hair growth in subjects with excessive, unwanted facial hair. After 24 weeks' treatment, 58% of eflornithine and 34% of placebo subjects have at least some improvement in facial hirsutism[3]. The hair growth inhibitory activity of eflornithine is significantly enhanced when the eflornithine cream is applied onto a mouse skin area pretreated with microneedles[4]. 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[5]. |
| Cell experiments | BY2 cells are treated with or without cryptogein in the presence or absence of DFMO(Difluoromethylornithine) and monitered the effect of chemicals on cell growth. (Only for Reference) |
| Synonyms | Difluoromethylornithine hydrochloride hydrate, α-difluoromethylornithine hydrochloride hydrate, 依氟鸟氨酸盐酸盐一水合物, Eflornithine hydrochloride, MDL-71782 hydrochloride hydrate, DFMO hydrochloride hydrate, RMI-71782 hydrochloride hydrate, Eflornithine hydrochloride Monohydrate |
| molecular weight | 236.64 |
| Molecular formula | C6H15ClF2N2O3 |
| CAS | 96020-91-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 55 mg/mL (232.42 mM) |
| References | 1. Yoda H, et al. Plant Physiol. 2006, 142(1):193-206. 2. Burri C, et al. Eflornithine for the treatment of human African trypanosomiasis. Parasitol Res. 2003 Jun;90 Supp 1:S49-52. 3. Balfour JA, et al. Topical eflornithine. Am J Clin Dermatol. 2001;2(3):197-201; discussion 202. 4. Kumar A, et al. A method to improve the efficacy of topical eflornithine hydrochloride cream. Drug Deliv. 2016 Jun;23(5):1495-501. 5. Lipke DW, et al. Eflornithine alters changes in vascular responsiveness associated with coarctation hypertension. Clin Exp Hypertens. 1997 Apr;19(3):297-312. 6. Dial C N. Modulation of Coxsackievirus Protease Activity by Polyamines[D]. Loyola University Chicago. 2019. 7. Dial C N, Tate P M, Kicmal T M, et al. Coxsackievirus B3 Responds to Polyamine Depletion via Enhancement of 2A and 3C Protease Activity[J]. Viruses. 2019 Apr 30;11(5). 8. Kicmal T M, Tate P M, Dial C N, et al. Polyamine depletion abrogates enterovirus cellular attachment[J]. Journal of virology. 2019, 93(20): e01054-19. 9. Mastrodomenico V, Esin J J, Graham M L, et al. Polyamine depletion inhibits bunyavirus infection via generation of noninfectious interfering virions[J]. Journal of virology. 2019 May 1. pii: JVI.00530-19. |
| Citations | 1. Mastrodomenico V, Esin J J, Graham M L, et al. Polyamine depletion inhibits bunyavirus infection via generation of noninfectious interfering virions. Journal of Virology. 2019 May 1. pii: JVI.00530-19 2. Kicmal T M, Tate P M, Dial C N, et al. Polyamine depletion abrogates enterovirus cellular attachment. Journal of Virology. 2019, 93(20): e01054-19 3. Dial C N, Tate P M, Kicmal T M, et al. Coxsackievirus B3 Responds to Polyamine Depletion via Enhancement of 2A and 3C Protease Activity. Viruses. 2019 Apr 30;11(5) 4. Firpo M R, LoMascolo N J, Petit M J, et al.Polyamines and eIF5A hypusination facilitate SREBP2 synthesis and cholesterol production leading to enhanced enterovirus attachment and infection.PLoS pathogens.2023, 19(4): e1011317. |
Eflornithine hydrochloride hydrate
CAS No.: 96020-91-6
Eflornithine hydrochloride hydrate (RMI-71782 hydrochloride hydrate) is a specific, irreversible inhibitor of ornithine
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