Size | Price | Stock | Qty |
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100mg |
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250mg |
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500mg |
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1g |
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2g |
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Other Sizes |
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Purity: ≥98%
Eflornithine HCl hydrate (DFMO; MDL71782; RMI71782; α-difluoromethylornithine) 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 |
Ornithine decarboxylase
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ln Vitro |
Eflornithine is a specific, irreversible inhibitor of the enzyme ornithine decarboxylase which is thought to slow hair growth by inhibiting this enzyme in hair follicles[2].
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ln Vivo |
The only novel drug approved in the last fifty years for the treatment of human African trypanosomiasis is eflornithine. It is mostly used as a stand-by medication for Trypanosoma brucei gambiense infections that do not respond to melarsoprol [1]. When it came to decreasing the growth of facial hair in participants with excess hair, eflornithine 15% cream outperformed a placebo. Following a 24-week course of treatment, face hirsutism improved at least somewhat in 58% of eflornithine patients and 34% of placebo subjects [2]. When eflornithine cream was administered to mouse skin areas that had been microneedled beforehand, the hair growth inhibitory activity of eflornithine was markedly increased [3]. After 14 days of hypertension, eflornithine treatment of constrictive hypertensive rats led to the normalization of KCI and norepinephrine contractile strength as well as the relaxing of acetylcholine [4].
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Enzyme Assay |
In in vitro studies using Salmonella and two strains of Saccharomyces, eflornithine did not induce mutagenic changes [1].
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Cell Assay |
In vitro permeation study of eflornithine was performed using Franz diffusion cell[3].
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Animal Protocol |
In vivo efficacy study was performed in a mouse model by monitoring the re-growth of hair in the lower dorsal skin of mice after the eflornithine cream was applied onto an area pretreated with microneedles. The skin and the hair follicles in the treated area were also examined histologically[3].
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References |
[1]. Burri C, et al. Eflornithine for the treatment of human African trypanosomiasis. Parasitol Res. 2003 Jun;90 Supp 1:S49-52.
[2]. Balfour JA, et al. Topical eflornithine. Am J Clin Dermatol. 2001;2(3):197-201; discussion 202. [3]. Kumar A, et al. A method to improve the efficacy of topical eflornithine hydrochloride cream. Drug Deliv. 2016 Jun;23(5):1495-501. [4]. Lipke DW, et al. Eflornithine alters changes in vascular responsiveness associated with coarctation hypertension. Clin Exp Hypertens. 1997 Apr;19(3):297-312 |
Molecular Formula |
C6H15CLF2N2O3
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Molecular Weight |
236.6447
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Exact Mass |
236.074
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Elemental Analysis |
C, 30.45; H, 6.39; Cl, 14.98; F, 16.06; N, 11.84; O, 20.28
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CAS # |
96020-91-6
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Related CAS # |
Eflornithine;70052-12-9;L-Eflornithine monohydrochloride;69955-42-6;Eflornithine hydrochloride;68278-23-9;L-Eflornithine;66640-93-5; 96020-91-6 (HCl hydrate) 68278-23-9 (HCl); 70050-55-4 (R-isomer); 69955-42-6 (S-isomer); 66640-93-5 (L-isomer)
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Appearance |
White to off-white solid powder
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LogP |
1.91
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tPSA |
98.57
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SMILES |
NC(CCCN)(C(F)F)C(O)=O.[H]Cl.[H]O[H]
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InChi Key |
FJPAMFNRCFEGSD-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C6H12F2N2O2.ClH.H2O/c7-4(8)6(10,5(11)12)2-1-3-9/h4H,1-3,9-10H2,(H,11,12)1H1H2
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Chemical Name |
2,5-diamino-2-(difluoromethyl)pentanoic acid hydrochloride hydrate
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Synonyms |
Ornidyl CPP-1X RMI71782 RMI-71782 RMI 71782
DL-Ornithine hydrochloride
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HS Tariff Code |
2934.99.9001
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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) |
H2O : ~83.33 mg/mL (~352.14 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (422.58 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
 (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 4.2258 mL | 21.1291 mL | 42.2583 mL | |
5 mM | 0.8452 mL | 4.2258 mL | 8.4517 mL | |
10 mM | 0.4226 mL | 2.1129 mL | 4.2258 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.