L-Eflornithine monohydrochloride (Synonyms: L-DFMO monohydrochloride; ; L-RMI71782 monohydrochloride; L-α-difluoromethylornithine monohydrochloride)

Name: L-Eflornithine monohydrochloride
Brand: MedChemExpress
SKU: HY-B0744D
Rating: 4.5 (1 reviews)

Cat. No.: HY-B0744D Purity: ≥98.0%: FAQs
Data Sheet SDS COA Handling Instructions

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L-Eflornithine monohydrochloride (L-DFMO monohydrochloride) is an enantiomer of Eflornithine. L-Eflornithine is an irreversible ornithine decarboxylase (ODC) inhibitor with a K_D of 1.3±0.3 µM, and a K_inact of 0.15±0.03 min^-1.

For research use only. We do not sell to patients.

L-Eflornithine monohydrochloride Chemical Structure

CAS No. : 69955-42-6

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10 mM * 1 mL in DMSO ready for reconstitution	USD 171	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 171	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

Other Forms of L-Eflornithine monohydrochloride:

Eflornithine hydrochloride hydrate In-stock
Eflornithine Get quote
Eflornithine hydrochloride Get quote
L-Eflornithine Get quote

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

KD:1.3±0.3 µM (Ornithine decarboxylase, ODC)^[1]

In Vitro

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 (K_D) 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 (K_inact) 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. 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^[1]. 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^[2].
The L-Eflornithine also appears to be more potent in cultured T.brucei gambiense parasites^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

218.63

Formula

C₆H₁₃ClF₂N₂O₂

CAS No.

69955-42-6

Appearance

Solid

Color

Light yellow to yellow

SMILES

N[C@](CCCN)(C(F)F)C(O)=O.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 200 mg/mL (914.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 50 mg/mL (228.70 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (22.87 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (22.87 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (22.87 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: ≥ 100 mg/mL (457.39 mM); Clear solution

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: ≥98.0%

Select Batch:

Data Sheet (273 KB) SDS (252 KB)

COA (247 KB) HNMR (261 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	4.5739 mL	22.8697 mL	45.7394 mL	114.3484 mL
	5 mM	0.9148 mL	4.5739 mL	9.1479 mL	22.8697 mL
	10 mM	0.4574 mL	2.2870 mL	4.5739 mL	11.4348 mL
	15 mM	0.3049 mL	1.5246 mL	3.0493 mL	7.6232 mL
	20 mM	0.2287 mL	1.1435 mL	2.2870 mL	5.7174 mL
	25 mM	0.1830 mL	0.9148 mL	1.8296 mL	4.5739 mL
	30 mM	0.1525 mL	0.7623 mL	1.5246 mL	3.8116 mL
	40 mM	0.1143 mL	0.5717 mL	1.1435 mL	2.8587 mL
	50 mM	0.0915 mL	0.4574 mL	0.9148 mL	2.2870 mL
	60 mM	0.0762 mL	0.3812 mL	0.7623 mL	1.9058 mL
	80 mM	0.0572 mL	0.2859 mL	0.5717 mL	1.4294 mL
	100 mM	0.0457 mL	0.2287 mL	0.4574 mL	1.1435 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

L-Eflornithine monohydrochloride Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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L-Eflornithine monohydrochloride69955-42-6L-DFMO monohydrochloride L-RMI71782 monohydrochlorideL-α-difluoromethylornithine monohydrochlorideParasiteInhibitorinhibitorinhibit

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L-Eflornithine monohydrochloride (Synonyms: L-DFMO monohydrochloride; ; L-RMI71782 monohydrochloride; L-α-difluoromethylornithine monohydrochloride)

Customer Review

Other Forms of L-Eflornithine monohydrochloride:

L-Eflornithine monohydrochloride Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Parasite Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

L-Eflornithine monohydrochloride Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

L-Eflornithine monohydrochloride Related Classifications

Keywords:

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