DFMO
DFMO Basic information
- Product Name:
- DFMO
- Synonyms:
-
- ALPHA-DIFLUORO-ME-DL-ORNITHINE
- ALPHA-DIFLUOROMETHYL-DL-ORNITHINE
- L-alpha-Difluoromethylornithine
- DFMO
- EFLORNITINE
- DL-ALPHA-DIFLUOROMETHYLORNITHINE
- DIFLUOROMETHYLORNITHINE
- H-DL-(F2ME)ORN-OH
- CAS:
- 66640-93-5
- MF:
- C6H12F2N2O2
- MW:
- 182.17
- Mol File:
- 66640-93-5.mol
DFMO Chemical Properties
- Boiling point:
- 347.0±42.0 °C(Predicted)
- Density
- 1.293±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- pka
- 1.22±0.44(Predicted)
DFMO Usage And Synthesis
Uses
L-Eflornithine (L-DFMO) is an enantiomer of Eflornithine. 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[1].
Biological Activity
L-Eflornithine (L-DFMO) is the enantiomer of Eflornithine. L-Eflornithine is an irreversible ornithine decarboxylase (ODC) inhibitor with KD of 1.3±0.3 μM and Kinact of 0.15±0.03 min-1.
in vivo
The more potent L-Eflornithine is present at much lower concentrations in both plasma and cerebrospinal fluid (CSF) than those of the D-Eflornithine. The plasma concentrations of L-Eflornithine are on average 52% of the D -enantiomer concentrations. The typical oral clearances of L-Eflornithine and D-eflornithine are 17.4 and 8.23 liters/h, respectively.
target
KD: 1.3±0.3 μM (Ornithine decarboxylase, ODC)
References
[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. DOI:10.1042/BJ20030382
[2] Jansson-L?fmark 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. DOI:10.1128/AAC.04101-14
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