Introduction：Basic information about CAS 70052-12-9|Eflornithine, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Eflornithine |
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| CAS Number | 70052-12-9 | Molecular Weight | 182.16800 |
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| Density | 1.293g/cm3 | Boiling Point | 347ºC at 760 mmHg |
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| Molecular Formula | C6H12F2N2O2 | Melting Point | / |
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| MSDS | / | Flash Point | 163.7ºC |
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Names
| Name | Eflornithine |
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| Synonym | More Synonyms |
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Eflornithine BiologicalActivity
| Description | Eflornithine is a specific, irreversible inhibitor of the enzyme ornithine decarboxylase. Eflornithine is a medication for the treatment of African trypanosomiasis and excessive facial hair growth in women. |
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| Related Catalog | Signaling Pathways >>Others >>OthersResearch Areas >>Others |
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| 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[1]. 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[2]. The hair growth inhibitory activity of eflornithine is significantly enhanced when the eflornithine cream is applied onto a mouse skin area pretreated with microneedles[3]. 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[4]. |
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| Animal Admin | Mice: The skin area where the hair is removed is then treated with the eflornithine hydrochloride 13.9% cream (∼50 mg per mouse per treatment) using a spatula 2 times a day in an interval of at least 8 h for a maximum period of 36 days[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. |
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Chemical & Physical Properties
| Density | 1.293g/cm3 |
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| Boiling Point | 347ºC at 760 mmHg |
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| Molecular Formula | C6H12F2N2O2 |
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| Molecular Weight | 182.16800 |
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| Flash Point | 163.7ºC |
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| Exact Mass | 182.08700 |
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| PSA | 89.34000 |
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| LogP | 1.17310 |
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| InChIKey | VLCYCQAOQCDTCN-UHFFFAOYSA-N |
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| SMILES | NCCCC(N)(C(=O)O)C(F)F |
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| Storage condition | 2-8℃ |
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Toxicological Information
CHEMICAL IDENTIFICATION - RTECS NUMBER :
- RM2981600
- CHEMICAL NAME :
- Ornithine, 2-(difluoromethyl)-
- CAS REGISTRY NUMBER :
- 70052-12-9
- LAST UPDATED :
- 199706
- DATA ITEMS CITED :
- 11
- MOLECULAR FORMULA :
- C6-H12-F2-N2-O2
- MOLECULAR WEIGHT :
- 182.20
- WISWESSER LINE NOTATION :
- Z3XZVQYFF
HEALTH HAZARD DATAACUTE TOXICITY DATA - TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human - man
- DOSE/DURATION :
- 800 mg/kg/4D-I
- TOXIC EFFECTS :
- Gastrointestinal - nausea or vomiting Blood - thrombocytopenia
- TYPE OF TEST :
- LDLo - Lowest published lethal dose
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Human - woman
- DOSE/DURATION :
- 67 mg/kg/40M-C
- TOXIC EFFECTS :
- Cardiac - cardiomyopathy including infarction Cardiac - pulse rate Vascular - BP lowering not characterized in autonomic section
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Human - man
- DOSE/DURATION :
- 9084 mg/kg/2W-I
- TOXIC EFFECTS :
- Gastrointestinal - nausea or vomiting Blood - thrombocytopenia
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Intraperitoneal
- DOSE :
- 1600 mg/kg
- SEX/DURATION :
- female 4-7 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- DOSE :
- 1 gm/kg
- SEX/DURATION :
- female 16-20 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Effects on Newborn - behavioral Reproductive - Effects on Newborn - physical
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- DOSE :
- 2500 mg/kg
- SEX/DURATION :
- female 15-17 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Specific Developmental Abnormalities - urogenital system Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - biochemical and metabolic
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- DOSE :
- 500 mg/kg
- SEX/DURATION :
- female 11-13 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Effects on Embryo or Fetus - other effects to embryo
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- DOSE :
- 2500 mg/kg
- SEX/DURATION :
- female 13-17 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Effects on Embryo or Fetus - other effects to embryo Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - physical
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Intrauterine
- DOSE :
- 50 ug/kg
- SEX/DURATION :
- female 4 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Fertility - other measures of fertility
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- DOSE :
- 800 mg/kg
- SEX/DURATION :
- female 8 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth)
MUTATION DATA - TEST SYSTEM :
- Rodent - rat
- DOSE/DURATION :
- 2800 mg/kg
- REFERENCE :
- BBACAQ Biochimica et Biophysica Acta. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1947- Volume(issue)/page/year: 696,179,1982
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Synonyms
| 2-(difluoromethyl)-2,5-diaminopentanoic acid |
| 2-(2-ethyl-2,3-dihydro-2-benzofuranyl)-4,5-dihydro-1H-imidazole hydrochloride |
| MFCD00242734 |
| 2,5-diamino-2-(difluoromethyl)pentanoic acid |
| 2-Ethyl-2-(imidazolin-2-yl)-2,3-dihydrobenzofuran hydrochloride |
| Efaroxan HCl |
| H-DL-(a-difluoromethyl)Orn-OH |
| Efaroxan hydrochloride |
