DFMO

Product NameDFMO
CAS66640-93-5
MFC6H12F2N2O2
MW182.17
EINECS
MOL File66640-93-5.mol

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)

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-Lfmark 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