< 生产厂家价格 >

盐酸依氟乌氨酸

盐酸依氟乌氨酸用途

Eflornithine hydrochloride是酶鸟氨酸脱羧酶的特异性不可逆抑制剂。Eflornithine是用于治疗非洲锥虫病和女性面部毛发过度生长的药物。

点击显示

盐酸依氟乌氨酸名称

[ CAS 号 ]:
68278-23-9

[ 中文名 ]:
盐酸依氟乌氨酸

[ 英文名 ]:
DFMO

[中文别名 ]:

盐酸依氟鸟氨酸

[英文别名 ]:

Eflornithine HCl Monohydrate
DFMO HCl
2-(Difluoromethyl)ornithine hydrochloride hydrate
dfmo
MFCD00274036
EINECS 269-532-0
EflornithineHcl
Eflornithine (hydrochloride)
2-(Difluoromethyl)-DL-ornithine monohydrochloride
DFMO hydrochloride hydrate

盐酸依氟乌氨酸生物活性

[ 描述 ]:

Eflornithine hydrochloride是酶鸟氨酸脱羧酶的特异性不可逆抑制剂。Eflornithine是用于治疗非洲锥虫病和女性面部毛发过度生长的药物。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 其他

[体内研究]

在过去的50年中,Eflornithine是唯一一种用于治疗非洲人类锥虫病的新分子。它主要用作melarsoprol难治性锥虫布氏锥虫病的后备药物[1]。在有过多的,不需要的面部毛发的受试者中,依维罗宁15％的乳膏在减少毛发生长方面优于安慰剂。治疗24周后,58％的依氟鸟氨酸和34％的安慰剂受试者在面部多毛症方面至少有一些改善[2]。当将依氟鸟氨酸乳膏应用于用微针预处理的小鼠皮肤区域时,eflornithine的毛发生长抑制活性显着增强[3]。用efl鸟嘌呤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,高血压14天后乙酰胆碱松弛[4]。

[动物实验]

小鼠：然后用盐酸依氟鸟氨酸13.9％乳膏（每次治疗每只小鼠约50mg）用刮刀每天2次，间隔至少8小时，最长36周期，处理除去毛发的皮肤区域。天[3]。

[参考文献]

[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.

[相关活性小分子]

盐酸依氟乌氨酸物理化学性质

[ 沸点 ]:
347ºC at 760 mmHg

[ 熔点 ]:
181-184°C

[ 分子式 ]:
C₆H₁₃ClF₂N₂O₂

[ 分子量 ]:
236.645

[ 闪点 ]:
163.7ºC

[ 精确质量 ]:
236.073929

[ PSA ]:
89.34000

[ LogP ]:
1.97510

[ 外观性状 ]:
白色固体

[ 水溶解性 ]:
H2O: >10 mg/mL, soluble

盐酸依氟乌氨酸毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: RM2981900

CHEMICAL NAME :: DL-Ornithine, 2-(difluoromethyl)-, monohydrochloride, hydrate

CAS REGISTRY NUMBER :: 68278-23-9

LAST UPDATED :: 199406

DATA ITEMS CITED :: 10

MOLECULAR FORMULA :: C6-H12-F2-N2-O2.Cl-H.H2-O

MOLECULAR WEIGHT :: 236.68

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 6,142,1981

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >3 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 6,142,1981

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 6,142,1981

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >3 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 6,142,1981 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1500 mg/kg

SEX/DURATION :: female 7-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

REFERENCE :: TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 35,55A,1987

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 11250 mg/kg

SEX/DURATION :: female 10-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death

REFERENCE :: TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 35,55A,1987

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2400 mg/kg

SEX/DURATION :: female 7-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - musculoskeletal system

REFERENCE :: TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 39,103,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 900 mg/kg

SEX/DURATION :: female 11-19 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

REFERENCE :: TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 35,55A,1987

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 9 gm/kg

SEX/DURATION :: female 11-19 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death

REFERENCE :: TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 35,55A,1987

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 260 mg/kg

SEX/DURATION :: female 7-19 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - musculoskeletal system

REFERENCE :: TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 39,103,1989

点击显示

盐酸依氟乌氨酸安全信息

[ WGK德国 ]:
3

[ 海关编码 ]:
2922499990

盐酸依氟乌氨酸海关

[ 海关编码 ]: 2922499990

[ 中文概述 ]:
2922499990 其他氨基酸及其酯及它们的盐（含有一种以上含氧基的除外）. 增值税率:17.0% 退税率:9.0% 监管条件:AB(入境货物通关单,出境货物通关单) 最惠国关税:6.5% 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乙醇胺及其盐应报明色度, 乙醇胺及其盐应报明包装

[ 监管条件 ]: A.入境货物通关单 B.出境货物通关单

[ 检验检疫 ]: P.进境动植物、动植物产品检疫 Q.出境动植物、动植物产品检疫 R.进口食品卫生监督检验 S.出口食品卫生监督检验 M.进口商品检验 N.出口商品检验

[ Summary ]:
HS:2922499990 other amino-acids, other than those containing more than one kind of oxygen function, and their esters; salts thereof VAT:17.0% Tax rebate rate:9.0% Supervision conditions:AB(certificate of inspection for goods inward,certificate of inspection for goods outward) MFN tariff:6.5% General tariff:30.0%