Ornithine decarboxylase

依氟鸟氨酸是鸟氨酸脱羧酶的一种特异性、不可逆的抑制剂，被认为通过抑制毛囊中的这种酶来减缓头发生长[2]。

过去五十年来唯一被批准用于治疗人类非洲锥虫病的新药是依氟鸟氨酸。它主要用作对 melarsoprol 没有反应的布氏冈比亚锥虫感染的备用药物 [1]。当谈到减少毛发过多的参与者面部毛发的生长时，15% 依氟鸟氨酸霜的效果优于安慰剂。经过 24 周的治疗疗程后，58% 的依氟鸟氨酸患者和 34% 的安慰剂受试者的面部多毛症至少有所改善 [2]。当将依氟鸟氨酸乳膏施用到预先经过微针处理的小鼠皮肤区域时，依氟鸟氨酸的毛发生长抑制活性显着增加[3]。高血压14天后，依氟鸟氨酸治疗缩窄性高血压大鼠导致KCI和去甲肾上腺素收缩强度正常化以及乙酰胆碱松弛[4]。

在使用沙门氏菌和两种酵母菌株的体外研究中，依氟鸟氨酸没有引起突变[1]。

使用Franz扩散池进行依氟鸟氨酸的体外渗透研究[3]。

In vivo efficacy study was performed in a mouse model by monitoring the re-growth of hair in the lower dorsal skin of mice after the eflornithine cream was applied onto an area pretreated with microneedles. The skin and the hair follicles in the treated area were also examined histologically[3].

Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
Maternal intravenous eflornithine 400 mg/kg daily for 7 days did not cause any adverse serious effects in breastfed infants. After topical application, eflornithine is poorly absorbed so it is not likely to reach the bloodstream of the infant or cause any adverse effects in breastfed infants.
◉ Effects in Breastfed Infants
A cohort of 33 infants who were breastfed (extent not stated) by hospitalized mothers taking nifurtimox was followed in the Democratic Republic of the Congo. Thirty mothers took a full course of 30 doses of oral nifurtimox 15 mg/kg daily and all received 14 doses of intravenous eflornithine 400 mg/kg daily for 7 days for human African trypanosomiasis. (sleeping sickness). Nursing mothers also took a median of 4 other concomitant medications, including amoxicillin, ciprofloxacin, metronidazole, trimethoprim-sulfamethoxazole, aspirin, and diclofenac (1 patient each); hydrocortisone, promethazine and quinine (2 patients each); levamisole (6 patients); sulfadoxine-pyrimethamine (8 patients); dipyrone (13 patients); acetaminophen (16 patients); and mebendazole (17 patients). No serious adverse events were reported in any of the breastfed infants.
◉ Effects on Lactation and Breastmilk
Relevant published information was not found as of the revision date.

[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

Eflornithine hydrochloride monohydrate is the hydrochloride and hydrate of the trypanocidal drug eflornithine. It is a hydrochloride and a hydrate. It contains an eflornithine.
Eflornithine Hydrochloride is the hydrochloride form of eflornithine, a difluoromethylated ornithine compound with antineoplastic activity. Eflornithine irreversibly inhibits ornithine decarboxylase, an enzyme required for polyamine biosynthesis, thereby inhibiting the formation and proliferation of tumor cells. Polyamines are involved in nucleosome oligomerization and DNA conformation, creating a chromatin environment that stimulates neoplastic transformation of cells. (NCI04)
An inhibitor of ornithine decarboxylase, the rate limiting enzyme of the polyamine biosynthetic pathway.
See also: Eflornithine (has active moiety).

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Drug Indication
Treatment of facial hirsutism in women.

C6H15CLF2N2O3

236.6447

236.074

C, 30.45; H, 6.39; Cl, 14.98; F, 16.06; N, 11.84; O, 20.28

96020-91-6

Eflornithine;70052-12-9;L-Eflornithine monohydrochloride;69955-42-6;Eflornithine hydrochloride;68278-23-9;L-Eflornithine;66640-93-5; 96020-91-6 (HCl hydrate) 68278-23-9 (HCl); 70050-55-4 (R-isomer); 69955-42-6 (S-isomer); 66640-93-5 (L-isomer)

441361

White to off-white solid powder

1.293g/cm3

347ºC at 760mmHg

>210ºC (dec.)

163.7ºC

1.91

98.57

5

7

5

14

166

0

Cl.O=C(C(C(F)F)(CCCN)N)O.O

FJPAMFNRCFEGSD-UHFFFAOYSA-N

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

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

Ornidyl CPP-1X RMI71782 RMI-71782 RMI 71782 DL-Ornithine hydrochloride

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

H2O : ~83.33 mg/mL (~352.14 mM)

配方 1 中的溶解度: 100 mg/mL (422.58 mM) in PBS (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液; 超声助溶。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。