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L-Eflornithine monohydrochloride

Name: L-Eflornithine monohydrochloride
Brand: TargetMol
SKU: T11812L
Rating: 4.5 (1 reviews)

(Synonyms: L-α-difluoromethylornithine monohydrochloride, L-RMI71782 monohydrochloride, L-DFMO monohydrochloride) Copy Product Info

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

Catalog No. T11812L Copy Product Info

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L-Eflornithine monohydrochloride 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 monohydrochloride (L-DFMO monohydrochloride) is an enantiomer of Eflornithine. L-Eflornithine is utilized in enzymology and polyamine biosynthesis research systems to investigate irreversible inhibition kinetics of ornithine decarboxylase, including enzyme inactivation parameters (KD and Kinact) and their relationship to catalytic turnover regulation in cellular metabolic models. L-Eflornithine monohydrochloride (L-DFMO monohydrochloride) is further applied in stereochemical and structure–activity relationship studies evaluating enantiomer-dependent enzyme binding and inhibition efficiency in biochemical assay systems.

Cas No. 69955-42-6

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Product Introduction

Bioactivity

Description	L-Eflornithine monohydrochloride 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 monohydrochloride (L-DFMO monohydrochloride) is an enantiomer of Eflornithine. L-Eflornithine is utilized in enzymology and polyamine biosynthesis research systems to investigate irreversible inhibition kinetics of ornithine decarboxylase, including enzyme inactivation parameters (KD and Kinact) and their relationship to catalytic turnover regulation in cellular metabolic models. L-Eflornithine monohydrochloride (L-DFMO monohydrochloride) is further applied in stereochemical and structure–activity relationship studies evaluating enantiomer-dependent enzyme binding and inhibition efficiency in biochemical assay systems.
Targets & IC50	Ornithine decarboxylase，ODC:1.3±0.3 µM (Kd)
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 (D/L-DFMO) is an inhibitor of ODC, the first enzyme in eukaryotic polyamine biosynthesis.?Both enantiomers of Eflornithine (DFMO) irreversibly inactivate ODC.?Both Eflornithine enantiomers (L-Eflornithine and D-Eflornithine) 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 of L-Eflornithine and D-Eflornithine are 17.4 and 8.23 liters/h, respectively. L-Eflornithine, being more potent, is present at 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 of the D-enantiomer.
Synonyms	L-α-difluoromethylornithine monohydrochloride, L-RMI71782 monohydrochloride, L-DFMO monohydrochloride

Chemical Properties

Molecular Weight	218.63
Formula	C₆H₁₃ClF₂N₂O₂
Cas No.	69955-42-6
Smiles	[C@@](CCCN)(C(F)F)(C(O)=O)N.Cl
Relative Density.	1.31g/cm3

Storage & Solubility Information

Storage

Keep away from moisture, Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: 40 mg/mL (182.96 mM), Sonication is recommended.

DMSO: 160 mg/mL (731.83 mM), Sonication is recommended.

Solution Preparation Table

H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	4.5739 mL	22.8697 mL	45.7394 mL	228.6969 mL
5 mM	0.9148 mL	4.5739 mL	9.1479 mL	45.7394 mL
10 mM	0.4574 mL	2.2870 mL	4.5739 mL	22.8697 mL
20 mM	0.2287 mL	1.1435 mL	2.2870 mL	11.4348 mL
50 mM	0.0915 mL	0.4574 mL	0.9148 mL	4.5739 mL
100 mM	0.0457 mL	0.2287 mL	0.4574 mL	2.2870 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

Ornithine decarboxylase,ODCL-α-difluoromethylornithineL-RMI-71782 MonohydrochlorideL-RMI-71782L-RMI71782L-RMI 71782 MonohydrochlorideL-RMI 71782L-Eflornithine MonohydrochlorideLEflornithine monohydrochlorideL-EflornithineL-DFMOL-alpha-difluoromethylornithine MonohydrochlorideL-alpha-difluoromethylornithineL-a-difluoromethylornithine MonohydrochlorideL-a-difluoromethylornithineL Eflornithine monohydrochloride

Related Tags: L-Eflornithine monohydrochloride chemical structure | L-Eflornithine monohydrochloride in vivo | L-Eflornithine monohydrochloride in vitro | L-Eflornithine monohydrochloride formula | L-Eflornithine monohydrochloride molecular weight