< 生产厂家价格 >

醋酸炔诺酮

醋酸炔诺酮用途

Norethindrone acetate是FDA批准用于治疗子宫内膜异位症,由异常激素水平引起的子宫出血症和继发性闭经的女性孕激素。

点击显示

醋酸炔诺酮名称

[ CAS 号 ]:
51-98-9

[ 中文名 ]:
炔诺酮醋酸酯

[ 英文名 ]:
19-Norethindrone acetate

[中文别名 ]:

[英文别名 ]:

17α-Ethinyl-19-nortestosterone acetate
NORLUTATE
17α-Ethynyl-19-nortestosterone acetate
19-Norethindrone acetate
17β-Acetoxy-19-nor-17α-pregn-4-en-20-yn-3-one
(17α)-3-Oxo-19-norpregn-4-en-20-yn-17-yl acetate
17-α-Ethynyl-19-nortestosterone acetate
17α-Ethinyl-19-nortestosterone-17β-acetate
Milligynon
MFCD04039850

醋酸炔诺酮生物活性

[ 描述 ]:

Norethindrone acetate是FDA批准用于治疗子宫内膜异位症,由异常激素水平引起的子宫出血症和继发性闭经的女性孕激素。

[ 相关类别 ]:

信号通路 >> 其他 >> 孕激素受体

研究领域 >> 心血管疾病

研究领域 >> 内分泌

研究领域 >> 炎症/免疫

[ 靶点 ]

Progesterone Receptor[1]

[体内研究]

醋酸炔诺酮可以是一种具有成本效益的替代方案,在治疗症状性子宫内膜异位症时具有相对轻微的副作用。用醋酸炔诺酮治疗的受试者获得痛经和非循环盆腔疼痛缓解[1]。单独使用醋酸炔诺酮是治疗子宫内膜异位症各阶段疼痛和出血的良好耐受性有效选择。无论先前的激素治疗方案如何,醋酸炔诺酮后出血评分均有所改善,并且所有患者的醋酸炔诺酮疼痛评分均有所改善,除了之前处方的GnRH激动剂加上加回[2]。醋酸炔诺酮在实验动物中显示出低的急性毒性,并且与人类中观察到的毒性缺乏一致。在几次人体剂量下单独向啮齿动物施用醋酸炔诺酮不会导致治疗相关的死亡率,血液学变化,行为改变或器官病变[3]。醋酸炔诺酮给药导致饲喂高碳水化合物饮食的大鼠的密度<1.006的血浆脂蛋白的甘油三酯,胆固醇和磷脂的浓度显着且成比例地降低。醋酸炔诺酮(0.1mM)也显着抑制棕榈酸和甘油掺入来自喂养大鼠的分离肝细胞的甘油三酯中[4]。

[动物实验]

大鼠：将雌性Sprague-Dawley大鼠（200-210g）（其中6只作为对照）分别笼养在上午9:00至晚上9:00照射的动物室中。喂食接受醋酸炔诺酮的7只大鼠中的每只大鼠35只。 μg/天，持续2周。水和含有高碳水化合物的大鼠食物可随意获取[4]。

[参考文献]

[1]. Muneyyirci-Delale O, et al. Effect of norethindrone acetate in the treatment of symptomatic endometriosis. Int J Fertil Womens Med. 1998 Jan-Feb;43(1):24-7.

[2]. Kaser DJ, et al. Use of norethindrone acetate alone for postoperative suppression of endometriosis symptoms. J Pediatr Adolesc Gynecol. 2012 Apr;25(2):105-8.

[3]. Maier WE, et al. Pharmacology and toxicology of ethinyl estradiol and norethindrone acetate in experimental animals. Regul Toxicol Pharmacol. 2001 Aug;34(1):53-61.

[4]. Cheng DC, et al. Norethindrone acetate inhibition of triglyceride synthesis and release by rat hepatocytes. Atherosclerosis. 1983 Jan;46(1):41-8.

[相关活性小分子]

醋酸炔诺酮物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
454.7±45.0 °C at 760 mmHg

[ 分子式 ]:
C₂₂H₂₈O₃

[ 分子量 ]:
340.456

[ 闪点 ]:
197.1±28.8 °C

[ 精确质量 ]:
340.203857

[ PSA ]:
43.37000

[ LogP ]:
3.99

[ 外观性状 ]:
固体;White to Almost white powder to crystal

[ 蒸汽压 ]:
0.0±1.1 mmHg at 25°C

[ 折射率 ]:
1.556

[ 储存条件 ]:
2~8°C

醋酸炔诺酮MSDS

详细MSDS(安全技术说明书)

醋酸炔诺酮毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: RC8965000

CHEMICAL NAME :: 19-Nor-17-alpha-pregn-4-en-20-yn-3-one, 17-acetoxy-

CAS REGISTRY NUMBER :: 51-98-9

BEILSTEIN REFERENCE NO. :: 2064104

LAST UPDATED :: 199612

DATA ITEMS CITED :: 37

MOLECULAR FORMULA :: C22-H28-O3

MOLECULAR WEIGHT :: 340.50

WISWESSER LINE NOTATION :: L E5 B666 OV MUTJ E1 FOV1 F1UU1 -B&EF

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 303 ug/kg/2Y-C

TOXIC EFFECTS :: Tumorigenic - equivocal tumorigenic agent by RTECS criteria Liver - tumors Nutritional and Gross Metabolic - weight loss or decreased weight gain

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2190 ug/kg

SEX/DURATION :: female 52 week(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2 mg/kg

SEX/DURATION :: female 20 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - menstrual cycle changes or disorders

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1150 ug/kg

SEX/DURATION :: female 23 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - other measures of fertility

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Implant

DOSE :: 45 ug/kg

SEX/DURATION :: lactating female 15 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Maternal Effects - postpartum

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Implant

DOSE :: 366 ug/kg

SEX/DURATION :: female 21 week(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

DOSE :: 15 mg/kg

SEX/DURATION :: female 13-30 week(s) after conception

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 12 mg/kg

SEX/DURATION :: female 1 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - other measures of fertility

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1 mg/kg

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

TOXIC EFFECTS :: Reproductive - Effects on Newborn - other neonatal measures or effects

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 6 mg/kg

SEX/DURATION :: female 1-3 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 408 mg/kg

SEX/DURATION :: female 30 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - menstrual cycle changes or disorders

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 7 mg/kg

SEX/DURATION :: female 14 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - uterus, cervix, vagina

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 1200 ug/kg

SEX/DURATION :: female 1 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - other measures of fertility

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 2800 ug/kg

SEX/DURATION :: female 14 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - ovaries, fallopian tubes

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 50 mg/kg

SEX/DURATION :: female 15-24 day(s) after conception

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 150 mg/kg

SEX/DURATION :: female 14-19 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - urogenital system Reproductive - Effects on Newborn - live birth index (measured after birth)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 55 mg/kg

SEX/DURATION :: female 15-25 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - extra-embryonic structures (e.g., placenta, umbilical cord) Reproductive - Specific Developmental Abnormalities - homeostasis

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 60 mg/kg

SEX/DURATION :: female 17-20 day(s) after conception

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 70 mg/kg

SEX/DURATION :: female 14 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - uterus, cervix, vagina

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Parenteral

DOSE :: 7500 ug/kg

SEX/DURATION :: female 1-3 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated) Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Implant

DOSE :: 25800 ug/kg

SEX/DURATION :: female 17 week(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) 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 :: Unreported

DOSE :: 2 ug/kg

SEX/DURATION :: female 1 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 80 mg/kg

SEX/DURATION :: female 16-19 day(s) after conception

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 20 mg/kg

SEX/DURATION :: female 1-4 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated) Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 4 mg/kg

SEX/DURATION :: female 5 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - uterus, cervix, vagina

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 3 mg/kg

SEX/DURATION :: female 3 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - other measures of fertility

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 125 ug/kg

SEX/DURATION :: female 1 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Implant

DOSE :: 7500 ug/kg

SEX/DURATION :: female 17 week(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea)

TYPE OF TEST :: Micronucleus test

TYPE OF TEST :: Sister chromatid exchange

TYPE OF TEST :: Dominant lethal test

MUTATION DATA

TEST SYSTEM :: Rodent - mouse

DOSE/DURATION :: 11200 mg/kg/4W

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 26,535,1974 *** REVIEWS *** IARC Cancer Review:Animal Sufficient Evidence IMSUDL IARC Monographs, Supplement. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) No.1- 1979- Volume(issue)/page/year: 7,294,1987 TOXICOLOGY REVIEW CMROCX Current Medical Research and Opinion. (Clayton-Wray Pub. Ltd., 1a High St., Alton, Hants., UK) V.1- 1972- Volume(issue)/page/year: 4,309,1976

点击显示

醋酸炔诺酮安全信息

[ 符号 ]:

GHS08

[ 信号词 ]:
Warning

[ 危害声明 ]:
H351

[ 警示性声明 ]:
P281

[ 个人防护装备 ]:
Eyeshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
Xn:Harmful

[ 风险声明 (欧洲) ]:
R40;R48

[ 安全声明 (欧洲) ]:
S36/37

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
RC8965000

[ 海关编码 ]:
2915299090

醋酸炔诺酮合成路线

详细合成路线

醋酸炔诺酮上下游产品

醋酸炔诺酮上游产品

醋酸炔诺酮下游产品

醋酸炔诺酮制备

以4-二甲基氨基吡啶(DMAP)为催化剂，使炔诺酮和醋酐反应，直接得到炔诺酮-17-醋酸酯.

点击显示

醋酸炔诺酮海关

[ 海关编码 ]: 2915299090

[ 中文概述 ]:
HS: 2915299090 其他乙酸盐退税率:9.0% 监管条件:AB(入境货物通关单,出境货物通关单) 增值税率:17.0% 最惠国关税:5.5% 普通关税:50.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ 监管条件 ]: A.入境货物通关单 B.出境货物通关单

[ 检验检疫 ]: 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 ]:
2915299090 salts of acetic acid。supervision conditions:AB(certificate of inspection for goods inward,certificate of inspection for goods outward)。VAT:17.0%。tax rebate rate:9.0%。MFN tariff:5.5%。general tariff:50.0%

醋酸炔诺酮文献

Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.

Chem. Res. Toxicol. 23 , 171-83, (2010)

Drug-induced liver injury is one of the main causes of drug attrition. The ability to predict the liver effects of drug candidates from their chemical structures is critical to help guide experimental...

Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.

Toxicol. Mech. Methods 18 , 217-27, (2008)

ABSTRACT Drug-induced phospholipidosis (PL) is a condition characterized by the accumulation of phospholipids and drug in lysosomes, and is found in a variety of tissue types. PL is frequently manifes...

Molecular modulation of estrogen-induced apoptosis by synthetic progestins in hormone replacement therapy: an insight into the women's health initiative study.

Cancer Res. 74(23) , 7060-8, (2014)

Hormone replacement therapy (HRT) is widely used to manage menopausal symptoms in women and can be comprised of an estrogen alone or an estrogen combined with a progestin. The Women's Health Initiativ...

更多文献

醋酸炔诺酮

醋酸炔诺酮用途

醋酸炔诺酮名称

醋酸炔诺酮生物活性

醋酸炔诺酮物理化学性质

醋酸炔诺酮MSDS

详细MSDS(安全技术说明书)

醋酸炔诺酮毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

醋酸炔诺酮安全信息

醋酸炔诺酮合成路线

详细合成路线

醋酸炔诺酮上下游产品

醋酸炔诺酮上游产品

醋酸炔诺酮下游产品

醋酸炔诺酮制备

醋酸炔诺酮海关

醋酸炔诺酮文献

相关化工产品/化学物质：

相关药品：

推荐生产厂家/供应商：

相关化合物