Eflornithine hydrochloride hydrate

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Chemical Structure| 96020-91-6 同义名 : DFMO hydrochloride hydrate;MDL-71782 hydrochloride hydrate;Eflornithine;DFMO;DL-α-Difluoromethylornithine (hydrochloride hydrate);Difluoromethylornithine hydrochloride hydrate;α-difluoromethylornithine hydrochloride hydrate;RMI-71782 hydrochloride hydrate
CAS号 : 96020-91-6
货号 : A102810
分子式 : C6H15ClF2N2O3
纯度 : 98%
分子量 : 236.645
MDL号 : MFCD00242734
存储条件：

Pure form Inert atmosphere,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

H2O: 85 mg/mL(359.19 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • decarboxylase
描述 Eflornithine hydrochloride hydrate is a specific, irreversible inhibitor of the enzyme ornithine decarboxylase. 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[3]. The hair growth inhibitory activity of eflornithine was significantly enhanced when the eflornithine cream was applied onto a mouse skin area pretreated with microneedles. Cell proliferation in the skin and hair follicles was also significantly inhibited when the eflornithine cream was applied onto a skin area pretreated with microneedles[4]. Treatment of coarctation hypertensive rats with eflornithine resulted in a normalization of the contractile intensity to KCI and norepinephrine and relaxations to acetylcholine by 14 days of hypertension. Normalization of vascular function can occur in the presence of significantly elevated blood pressure upon chronic administration of eflornithine[5]. Male SD rats were administered single doses of racemic eflornithine hydrochloride as an oral solution (750, 1,500, 2,000, or 3,000 mg/kg of body weight) or intravenously (375 or 1,000 mg/kg of body weight). The mean bioavailabilities for L- and D-eflornithine were 41% and 62%, respectively, in the dose range of 750 to 2,000 mg/kg of body weight, with suggested increases to 47% and 83%, respectively, after a dose of 3,000 mg/kg of body weight[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.23mL

0.85mL

0.42mL

21.13mL

4.23mL

2.11mL

42.26mL

8.45mL

4.23mL
参考文献

[1]Kumar A, Naguib YW, et al. A method to improve the efficacy of topical eflornithine hydrochloride cream. Drug Deliv. 2016 Jun;23(5):1495-501.

[2]Balfour JA, McClellan K. Topical eflornithine. Am J Clin Dermatol. 2001;2(3):197-201; discussion 202.

[3]Balfour JA, McClellan K. Topical eflornithine. Am J Clin Dermatol. 2001;2(3):197-201; discussion 202

[4]Kumar A, Naguib YW, Shi YC, Cui Z. A method to improve the efficacy of topical eflornithine hydrochloride cream. Drug Deliv. 2016 Jun;23(5):1495-501

[5]Lipke DW, Newman PS, Tofiq S, Aziz SM, Soltis EE. Eflornithine alters changes in vascular responsiveness associated with coarctation hypertension. Clin Exp Hypertens. 1997 Apr;19(3):297-312

[6]Jansson R, Malm M, Roth C, Ashton M. Enantioselective and nonlinear intestinal absorption of eflornithine in the rat. Antimicrob Agents Chemother. 2008 Aug;52(8):2842-8