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Eflornithine hydrochloride (DFMO hydrochloride) Sale

(Synonyms: 依氟鸟氨酸,DFMO hydrochloride; MDL71782 hydrochloride; RMI71782 hydrochloride; α-difluoromethylornithine hydrochloride) 目录号 : GC30308

Eflornithine hydrochloride (DFMO hydrochloride) 是一种特异性的、不可逆的鸟氨酸脱羧酶抑制剂。

Eflornithine hydrochloride (DFMO hydrochloride) Chemical Structure

Cas No.:68278-23-9

规格 价格 库存
10mg
¥457.00
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50mg
¥848.00
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Sample solution is provided at 25 µL, 10mM.

Description

Eflornithine hydrochloride 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.

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].

[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.

实验参考方法

Animal experiment:

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].

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.

化学性质

Cas No. 68278-23-9 SDF
别名 依氟鸟氨酸,DFMO hydrochloride; MDL71782 hydrochloride; RMI71782 hydrochloride; α-difluoromethylornithine hydrochloride
Canonical SMILES NC(CCCN)(C(F)F)C(O)=O.[H]Cl
分子式 C6H13ClF2N2O2 分子量 218.63
溶解度 ≥ 11.55mg/mL in Water 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 4.5739 mL 22.8697 mL 45.7394 mL
5 mM 0.9148 mL 4.5739 mL 9.1479 mL
10 mM 0.4574 mL 2.287 mL 4.5739 mL
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