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L-Eflornithine, the L-enantiomer of Eflornithine (DFMO; MDL71782; RMI71782; α-difluoromethylornithine) which is a potent, specific, irreversible inhibitor of the enzyme ornithine decarboxylase. Eflornithine is used as a medication for the treatment of African trypanosomiasis and excessive facial hair growth in women. Facial hirsutism is a cosmetic concern for women and can lead to significant anxiety and lack of self-esteem. Eflornithine cream is indicated for the treatment of facial hirsutism. However, limited success rate and overall patient's satisfaction, even with a long-term and high-frequency application, leave room for improvement.
| ln Vitro |
Eflornithine (D/L-DFMO) is an inhibitor of ODC, the first enzyme in eukaryotic polyamine production. Both enantiomers of eflornithine (DFMO) irreversibly inactivate ODC. Two eflornithine enantiomers (L-eflornithine and D-eflornithine) decrease ODC activity in a time- and concentration-dependent manner. The inhibitor dissociation constant (KD) values of D-eflornithine, L-eflornithine and eflornithine producing enzyme-inhibitor complexes are 28.3±3.4, 1.3±0.3 and 2.2± respectively. 0.4 µM. The inhibitor deactivation constants (Kinact) for the irreversible phase were 0.25±0.03, 0.15±0.03 and 0.15±0.03 min-1 for D-Eflornithine, L-Eflornithine and Eflornithine, respectively. Treatment of human colon tumor-derived HCT116 cells with L-eflornithine or D-eflornithine lowers cellular polyamine levels in a concentration-dependent manner [1]. Enantiomers exhibit varied potencies in vitro, with the L-enantiomer having a 20-fold greater affinity for the target enzyme ornithine decarboxylase [2]. L-eflornithine also appears to be more efficient against cultured parasites of B. gambiae [2].
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| ln Vivo |
Compared to D-eflornithine, the more potent L-eflornithine is found in significantly lower amounts in plasma and cerebrospinal fluid (CSF). L-eflornithine's typical plasma concentration is 52% of the D-enantiomer's concentration. L-eflornithine and D-eflornithine had typical oral clearance rates of 17.4 L/h and 8.23 L/h, respectively [2].
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| 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.
[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. |
| Molecular Formula |
C₆H₁₃CLF₂N₂O₂
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|---|---|
| Molecular Weight |
218.63
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| CAS # |
69955-42-6
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| Related CAS # |
Eflornithine;70052-12-9;Eflornithine hydrochloride hydrate;96020-91-6;Eflornithine hydrochloride;68278-23-9;L-Eflornithine;66640-93-5
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| SMILES |
N[C@](CCCN)(C(F)F)C(O)=O.Cl
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| Synonyms |
L-DFMO (monohydrochloride L-RMI71782 (monohydrochloride L-α-difluoromethylornithine (monohydrochloride
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~200 mg/mL (~914.79 mM)
H2O : ~50 mg/mL (~228.70 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (22.87 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (22.87 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5 mg/mL (22.87 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 100 mg/mL (457.39 mM) (saturation unknown) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.5739 mL | 22.8697 mL | 45.7394 mL | |
| 5 mM | 0.9148 mL | 4.5739 mL | 9.1479 mL | |
| 10 mM | 0.4574 mL | 2.2870 mL | 4.5739 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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