Eflornithine HCl hydrate (DFMO; MDL71782; RMI71782)

Alias: Ornidyl CPP-1X RMI71782 RMI-71782 RMI 71782 DL-Ornithine hydrochloride
Cat No.:V17490 Purity: ≥98%
EflornithineHCl hydrate (DFMO; MDL71782; RMI71782; α-difluoromethylornithine) is a potent, specific, irreversible inhibitor of the enzymeornithine decarboxylase.
Eflornithine HCl hydrate (DFMO; MDL71782; RMI71782) Chemical Structure CAS No.: 96020-91-6
Product category: Decarboxylase
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
100mg
250mg
500mg
1g
2g
Other Sizes

Other Forms of Eflornithine HCl hydrate (DFMO; MDL71782; RMI71782):

  • Eflornithine (DFMO; MDL71782; RMI71782)
  • L-Eflornithine monohydrochloride
  • Eflornithine HCl
  • L-Eflornithine
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

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.

Biological Activity I Assay Protocols (From Reference)
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].
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
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C6H15CLF2N2O3
Molecular Weight
236.6447
CAS #
96020-91-6
Related CAS #
Eflornithine;70052-12-9;L-Eflornithine monohydrochloride;69955-42-6;Eflornithine hydrochloride;68278-23-9;L-Eflornithine;66640-93-5
SMILES
NC(CCCN)(C(F)F)C(O)=O.[H]Cl.[H]O[H]
InChi Key
FJPAMFNRCFEGSD-UHFFFAOYSA-N
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
Chemical Name
2,5-diamino-2-(difluoromethyl)pentanoic acid hydrochloride hydrate
Synonyms
Ornidyl CPP-1X RMI71782 RMI-71782 RMI 71782 DL-Ornithine hydrochloride
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)
Solubility Data
Solubility (In Vitro)
H2O : ~83.33 mg/mL (~352.14 mM)
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.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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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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