| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
Eflornithine hydrochloride 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.
| Targets |
Trypanosoma
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|---|---|
| ln Vivo |
The only novel drug approved in the past 50 years to treat human African trypanosomiasis is eflornithine. This medication is primarily used as a backup in cases of Trypanosoma brucei gambiense that are resistant to melarsoprol[1]. If a subject has excessive, undesired facial hair, eflornithine 15% cream works better at reducing hair growth than a placebo. Following a 24-week course of treatment, facial hirsutism has improved at least somewhat in 58% of eflornithine subjects and 34% of placebo subjects[2]. When eflornithine cream is applied to a mouse skin area that has been pretreated with microneedles, its hair growth inhibitory activity is greatly increased[3]. After 14 days of hypertension, eflornithine treatment of coarctation hypertensive rats causes the contractile intensity to return to normal in response to KCI and norepinephrine, and the relaxation response to acetylcholine[4].
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| Animal Protocol |
Mice: For a maximum of 36 days, the skin area where the hair is removed is then treated with eflornithine hydrochloride 13.9% cream (approximately 50 mg per mouse per treatment) using a spatula twice a day at least 8 hours apart[3].
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| References |
| Molecular Formula |
C6H12N2O2F2.HCL
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|---|---|
| Molecular Weight |
218.62942
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| CAS # |
68278-23-9
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| Related CAS # |
Eflornithine;70052-12-9;Eflornithine hydrochloride hydrate;96020-91-6;L-Eflornithine monohydrochloride;69955-42-6;L-Eflornithine;66640-93-5
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| SMILES |
NC(CCCN)(C(F)F)C(O)=O.[H]Cl
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| InChi Key |
VKDGNNYJFSHYKD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C6H12F2N2O2.ClH/c7-4(8)6(10,5(11)12)2-1-3-9;/h4H,1-3,9-10H2,(H,11,12);1H
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| Chemical Name |
2,5-diamino-2-(difluoromethyl)pentanoic acid;hydrochloride
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| Synonyms |
DFMO hydrochloride; MDL71782 hydrochloride; RMI71782 hydrochloride; α-difluoromethylornithine hydrochloride; MDL-71782 hydrochloride; RMI-71782 hydrochloride; α-difluoromethylornithine hydrochloride; MDL 71782 hydrochloride; RMI 71782 hydrochloride; α-difluoromethylornithine hydrochloride
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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 Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| 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.
 Digital photographs of C57BL/6 mouse dorsal skin with and without treatment with the Vaniqa eflornithine cream (13.9%) for up to 36 days. |
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 In vitropermeation of eflornithine hydrochloride in a solution through a mouse skin area where the hair was trimmed (without microneedle), or trimmed and then treated with microneedles (with microneedle). Data shown are mean ± S.D. (n = 3).Drug Deliv.2016 Jun;23(5):1495-501. |
 Representative micrographic pictures of skin samples after anti-BrdU staining (A) or H&E staining (B). Scale bar = 2 mm.Drug Deliv.2016 Jun;23(5):1495-501. |
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