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L-Eflornithine

Catalog No. T11812 CAS 66640-93-5

Synonyms: L-α-difluoromethylornithine, L-RMI71782, L-DFMO

L-Eflornithine is an irreversible ornithine decarboxylase (ODC) inhibitor with a KD of 1.3±0.3 μM, and a Kinact of 0.15±0.03 min-1. L-Eflornithine is an enantiomer of Eflornithine.

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L-Eflornithine, CAS 66640-93-5

Pack Size	Availability	Price/USD
25 mg	6-8 weeks	$ 1,520.00
50 mg	6-8 weeks	$ 1,980.00
100 mg	6-8 weeks	$ 2,500.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	L-Eflornithine is an irreversible ornithine decarboxylase (ODC) inhibitor with a KD of 1.3±0.3 μM, and a Kinact of 0.15±0.03 min-1. L-Eflornithine is an enantiomer of Eflornithine.
Targets&IC50	Ornithine decarboxylase，ODC:(kd)1.3±0.3 µM
In vitro	Treatment of human colon tumour-derived HCT116 cells with either L-Eflornithine or D- Eflornithine decreases the cellular polyamine contents in a concentration-dependent manner. The enantiomers display different potencies in vitro, with the L-enantiomer having up to a 20-fold higher affinity for the target enzyme ornithine decarboxylase. ?The L-Eflornithine also appears to be more potent in cultured T.brucei gambiense parasites.?Eflornithine ?is an inhibitor of ODC, the first enzyme in eukaryotic polyamine biosynthesis.?Both enantiomers of Eflornithine ?irreversibly inactivate ODC.?Both Eflornithine enantiomers ?suppress ODC activity in a time- and concentration-dependent manner.?The inhibitor dissociation constant (KD) values for the formation of enzyme-inhibitor complexes are 28.3±3.4, 1.3±0.3 and 2.2±0.4 μM respectively for D-Eflornithine, L-Eflornithine and Eflornithine.?The inhibitor inactivation constants (Kinact) for the irreversible step were 0.25±0.03, 0.15±0.03 and 0.15±0.03 min-1 respectively for D-Eflornithine, L-Eflornithine and Eflornithine.
In vivo	The typical oral clearances for L-Eflornithine and D-eflornithine are 17.4 and 8.23 liters/hour, respectively. Despite L-Eflornithine being the more potent form, it is found in significantly lower concentrations in both plasma and cerebrospinal fluid (CSF) compared to D-Eflornithine. On average, plasma concentrations of L-Eflornithine are 52% of those found for the D-enantiomer.

Synonyms	L-α-difluoromethylornithine, L-RMI71782, L-DFMO
Molecular Weight	182.17
Formula	C6H12F2N2O2
CAS No.	66640-93-5

Storage

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

References and Literature

1. Qu N, et al. Inhibition of human ornithine decarboxylase activity by enantiomers of difluoromethylornithine. Biochem J. 2003 Oct 15;375(Pt 2):465-70. 2. Jansson-Löfmark R, et al. Enantiospecific reassessment of the pharmacokinetics and pharmacodynamics of oral eflornithine against late-stage Trypanosoma brucei gambiense sleeping sickness. Antimicrob Agents Chemother. 2015 Feb;59(2):1299-307. 3. Hulsebosch B M, Mounce B C. Polyamine Analog Diethylnorspermidine Restricts Coxsackievirus B3 and Is Overcome by 2A Protease Mutation In Vitro[J]. Viruses. 2021, 13(2): 310.

Citations

1. Mastrodomenico V, LoMascolo N J, Cruz-Pulido Y E, et al. Polyamine-Linked Cholesterol Incorporation in Rift Valley Fever Virus Particles Promotes Infectivity. ACS Infectious Diseases. 2022 2. Hulsebosch B M, Mounce B C. Polyamine Analog Diethylnorspermidine Restricts Coxsackievirus B3 and Is Overcome by 2A Protease Mutation In Vitro. Viruses. 2021 Feb 16;13(2):310. doi: 10.3390/v13020310.

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Keywords

L-Eflornithine 66640-93-5 Others L Eflornithine L-RMI-71782 LEflornithine L-RMI 71782 L-a-difluoromethylornithine L-α-difluoromethylornithine L-alpha-difluoromethylornithine L-RMI71782 L-DFMO inhibitor inhibit

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