Eflornithine HCl H2O

Eflornithine HCl is a specific, irreversible inhibitor of the enzyme ornithine decarboxylase, is a medication for the treatment of African trypanosomiasis and excessive facial hair growth in women.

Product information

CAS Number: 96020-91-6

Molecular Weight: 236.64

Formula: C6H15ClF2N2O3

Synonym:

DFMO hydrochloride hydrate

MDL-71782 hydrochloride hydrate

RMI-71782 hydrochloride hydrate

α-difluoromethylornithine hydrochloride hydrate

Chemical Name: 2,5-diamino-2-(difluoromethyl)pentanoic acid hydrochloride hydrate

Smiles: O.Cl.NCCCC(N)(C(F)F)C(O)=O

InChiKey: FJPAMFNRCFEGSD-UHFFFAOYSA-N

InChi: 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);1H;1H2

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: Insoluble. Water: 47 mg/mL(198.61 mM).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vivo:

Eflornithine is the only new molecule registered for the treatment of human African trypanosomiasis over the last 50 years. It is the drug used mainly as a back-up for melarsoprol refractory Trypanosoma brucei gambiense cases. In subjects with excessive, unwanted facial hair, eflornithine 15% cream is superior to placebo in reducing hair growth. After 24 weeks' treatment, 58% of eflornithine and 34% of placebo subjects have at least some improvement in facial hirsutism. The hair growth inhibitory activity of eflornithine is significantly enhanced when the eflornithine cream is applied onto a mouse skin area pretreated with microneedles. Treatment of coarctation hypertensive rats with eflornithine results in a normalization of the contractile intensity to KCI and norepinephrine and relaxations to acetylcholine by 14 days of hypertension.

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.

Products are for research use only. Not for human use.