米非司酮
米非司酮用途
米非司酮名称
[ CAS 号 ]:
84371-65-3
[ 中文名 ]:
米非司酮
[ 英文名 ]:
Mifepristone
[中文别名 ]:
[英文别名 ]:
- RU486
- MFCD00867226
- RU-486
- Mifepristone
- Mifestone
米非司酮生物活性
[ 描述 ]:
[ 相关类别 ]:
[ 靶点 ]
IC50: 0.2 nM (progesterone receptor, in T47D cells), 2.6 nM (glucocorticoid receptor, in A549 cells)[1]
[体外研究]
[体内研究]
[激酶实验]
[细胞实验]
[动物实验]
[参考文献]
[相关活性小分子]
米非司酮物理化学性质
[ 密度 ]:
1.2±0.1 g/cm3
[ 沸点 ]:
628.6±55.0 °C at 760 mmHg
[ 熔点 ]:
195-198°C
[ 分子式 ]:
C29H35NO2
[ 分子量 ]:
429.594
[ 闪点 ]:
334.0±31.5 °C
[ 精确质量 ]:
429.266785
[ PSA ]:
40.54000
[ LogP ]:
4.95
[ 外观性状 ]:
淡黄色固体
[ 蒸汽压 ]:
0.0±1.9 mmHg at 25°C
[ 折射率 ]:
1.623
[ 储存条件 ]:
2-8°C
[ 水溶解性 ]:
可溶于:氯仿
米非司酮MSDS
米非司酮毒性和生态
CHEMICAL IDENTIFICATION
- RTECS NUMBER :
- KG2955000
- CHEMICAL NAME :
- Estra-4,9-dien-3-one, 11-(4-(dimethylamino)phenyl)-17-hydroxy-17-(1-propyny l)-, (11-beta, 17-beta)-
- CAS REGISTRY NUMBER :
- 84371-65-3
- LAST UPDATED :
- 199709
- DATA ITEMS CITED :
- 26
- MOLECULAR FORMULA :
- C29-H35-N-O2
- MOLECULAR WEIGHT :
- 429.65
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 12 mg/kg
- SEX/DURATION :
- female 7 week(s) after conception
- TOXIC EFFECTS :
- Reproductive - Fertility - abortion
- REFERENCE :
- FESTAS Fertility and Sterility. (American Fertility Soc., 608 13th Ave. S, Birmingham, AL 35282) V.1- 1950- Volume(issue)/page/year: 56,32,1991
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 14 mg/kg
- SEX/DURATION :
- female 7-8 week(s) after conception
- TOXIC EFFECTS :
- Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)
- REFERENCE :
- CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1- 1970- Volume(issue)/page/year: 35,307,1987
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 12 mg/kg
- SEX/DURATION :
- female 6 week(s) after conception
- TOXIC EFFECTS :
- Reproductive - Fertility - abortion
- REFERENCE :
- EOGRAL European Journal of Obstetrics, Gynecology and Reproductive Biology. (Elsevier Science Pub. BV, POB 211, 1000 AE Amsterdam, Netherlands) V.3- 1973- Volume(issue)/page/year: 28,249,1988
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 12 mg/kg
- SEX/DURATION :
- female 10 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Fertility - abortion
- REFERENCE :
- OBGNAS Obstetrics and Gynecology. (Elsevier Science Pub. Co., Inc., 52 Vanderbilt Ave., New York, NY 10017) V.1- 1953- Volume(issue)/page/year: 74,653,1989
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 10 mg/kg
- SEX/DURATION :
- female 6 week(s) after conception
- TOXIC EFFECTS :
- Reproductive - Maternal Effects - other effects Reproductive - Fertility - abortion
- REFERENCE :
- GOBIDS Gynecologic and Obstetric Investigation. (S. Karger Pub., Inc., 79 Fifth Ave., New York, NY 10003) V.9- 1978- Volume(issue)/page/year: 29,13,1990
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 12 mg/kg
- SEX/DURATION :
- female 6-8 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) Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)
- REFERENCE :
- CYLPDN Zhongguo Yaoli Xuebao. Acta Pharmacologica Sinica. Chinese Journal of Pharmacology. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1980- Volume(issue)/page/year: 14,437,1993
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 160 mg/kg
- SEX/DURATION :
- female 1-20 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)
- REFERENCE :
- BMEMDK Biological Memoirs. (International Publishers, C 131, Mahanagar, Lucknow 226 006, India) V.1- 1976- Volume(issue)/page/year: 15,107,1989
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 12 mg/kg
- SEX/DURATION :
- female 7-9 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated)
- REFERENCE :
- SCYYDZ Shengzhi Yu Biyun. Reproduction and Contraception. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) 1980- Volume(issue)/page/year: 15,47,1995
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 6250 ug/kg
- SEX/DURATION :
- female 7 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Maternal Effects - uterus, cervix, vagina Reproductive - Fertility - abortion
- REFERENCE :
- SCYYDZ Shengzhi Yu Biyun. Reproduction and Contraception. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) 1980- Volume(issue)/page/year: 14,332,1994
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Administration onto the skin
- DOSE :
- 50 mg/kg
- SEX/DURATION :
- female 21 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Maternal Effects - parturition Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
- REFERENCE :
- JRPFA4 Journal of Reproduction and Fertility. (Biochemical Soc. Book Depot, POB 32, Commerce Way, Colchester, Essex CO2 8HP, UK) V.1- 1960- Volume(issue)/page/year: 79,1,1987
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- DOSE :
- 2500 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)
- REFERENCE :
- JRPFA4 Journal of Reproduction and Fertility. (Biochemical Soc. Book Depot, POB 32, Commerce Way, Colchester, Essex CO2 8HP, UK) V.1- 1960- Volume(issue)/page/year: 80,487,1987
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- DOSE :
- 10 mg/kg
- SEX/DURATION :
- female 1-2 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Fertility - other measures of fertility
- REFERENCE :
- JRPFA4 Journal of Reproduction and Fertility. (Biochemical Soc. Book Depot, POB 32, Commerce Way, Colchester, Essex CO2 8HP, UK) V.1- 1960- Volume(issue)/page/year: 80,487,1987
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- DOSE :
- 45 mg/kg
- SEX/DURATION :
- female 5-7 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Maternal Effects - other effects Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Fertility - other measures of fertility
- REFERENCE :
- JRPFA4 Journal of Reproduction and Fertility. (Biochemical Soc. Book Depot, POB 32, Commerce Way, Colchester, Essex CO2 8HP, UK) V.1- 1960- Volume(issue)/page/year: 83,73,1988
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- DOSE :
- 30 mg/kg
- SEX/DURATION :
- female 2 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) Reproductive - Maternal Effects - other effects
- REFERENCE :
- JRPFA4 Journal of Reproduction and Fertility. (Biochemical Soc. Book Depot, POB 32, Commerce Way, Colchester, Essex CO2 8HP, UK) V.1- 1960- Volume(issue)/page/year: 83,279,1988
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 200 mg/kg
- SEX/DURATION :
- female 1-2 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) Reproductive - Effects on Embryo or Fetus - cytological changes (including somatic cell genetic material) Reproductive - Effects on Embryo or Fetus - other effects to embryo
- REFERENCE :
- CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1- 1970- Volume(issue)/page/year: 41,551,1990
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 6 mg/kg
- SEX/DURATION :
- female 6-8 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) Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)
- REFERENCE :
- CYLPDN Zhongguo Yaoli Xuebao. Acta Pharmacologica Sinica. Chinese Journal of Pharmacology. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1980- Volume(issue)/page/year: 14,437,1993
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 3 mg/kg
- SEX/DURATION :
- female 7-9 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated)
- REFERENCE :
- SCYYDZ Shengzhi Yu Biyun. Reproduction and Contraception. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) 1980- Volume(issue)/page/year: 15,47,1995
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- DOSE :
- 4 mg/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)
- REFERENCE :
- CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1- 1970- Volume(issue)/page/year: 36,549,1987
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- DOSE :
- 2 mg/kg
- SEX/DURATION :
- female 15 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)
- REFERENCE :
- JRPFA4 Journal of Reproduction and Fertility. (Biochemical Soc. Book Depot, POB 32, Commerce Way, Colchester, Essex CO2 8HP, UK) V.1- 1960- Volume(issue)/page/year: 96,299,1992
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- DOSE :
- 2 mg/kg
- SEX/DURATION :
- female 7 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated)
- REFERENCE :
- CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1- 1970- Volume(issue)/page/year: 47,317,1993
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- DOSE :
- 400 ug/kg
- SEX/DURATION :
- female 7 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Maternal Effects - other effects
- REFERENCE :
- CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1- 1970- Volume(issue)/page/year: 47,317,1993
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 22500 ug/kg
- SEX/DURATION :
- female 32-36 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Maternal Effects - other effects Endocrine - changes in luteinizing hormone Reproductive - Fertility - abortion
- REFERENCE :
- JRPFA4 Journal of Reproduction and Fertility. (Biochemical Soc. Book Depot, POB 32, Commerce Way, Colchester, Essex CO2 8HP, UK) V.1- 1960- Volume(issue)/page/year: 88,99,1990
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 70 mg/kg
- SEX/DURATION :
- female 32-39 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Fertility - abortion
- REFERENCE :
- CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1- 1970- Volume(issue)/page/year: 41,85,1990
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Intramuscular
- DOSE :
- 10 mg/kg
- SEX/DURATION :
- female 15-18 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)
- REFERENCE :
- JMPMAO Journal of Medical Primatology. (Munksgaard International Publishers, 238 Main St., Cambridge, MA 02142) V.1- 1972- Volume(issue)/page/year: 23,319,1994
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Intramuscular
- DOSE :
- 8 mg/kg
- SEX/DURATION :
- female 21 week(s) after conception
- TOXIC EFFECTS :
- Reproductive - Maternal Effects - parturition Endocrine - effect on menstrual cycle
- REFERENCE :
- JRPFA4 Journal of Reproduction and Fertility. (Biochemical Soc. Book Depot, POB 32, Commerce Way, Colchester, Essex CO2 8HP, UK) V.1- 1960- Volume(issue)/page/year: 97,233,1993 *** REVIEWS *** TOXICOLOGY REVIEW HUREEE Human Reproduction. (IRL Press Inc., POB Q, McLean, VA 22101) V.1- 1986- Volume(issue)/page/year: 1,107,1986
米非司酮安全信息
[ 符号 ]:
GHS08
[ 信号词 ]:
Danger
[ 危害声明 ]:
H360
[ 警示性声明 ]:
P201-P280-P308 + P313
[ 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) ]:
T: Toxic;
[ 风险声明 (欧洲) ]:
R60
[ 安全声明 (欧洲) ]:
S53-S22-S36/37/39-S45
[ 危险品运输编码 ]:
NONH for all modes of transport
[ WGK德国 ]:
3
[ RTECS号 ]:
KG2955000
米非司酮上下游产品
米非司酮上游产品
米非司酮下游产品
米非司酮制备
方法1:以4,9雌甾二烯-3,17-二酮的3位缩酮化合物(Ⅰ)为原料,和丙炔溴化镁格氏试剂反应,在17位引入丙炔基,得到化合物(Ⅱ)。接着对5位烯键进行选择性环氧化,得化合物(Ⅲ)。然后在含溴化铜-甲硫醚络合物的四氢呋喃中,和对二甲氨基苯溴化镁反应,在11位引入对二甲氨基苯基,得化合物(Ⅳ)。最后在甲醇中,用盐酸水解并脱水,得到米非司酮。收率21.5%。
方法2:同样以4,9-雌甾二烯-3,17-二酮为原料,对3位羰基进行保护;然后先环氧化,再在17位引入丙炔基,在11位引入对二甲氨基苯基,最后水解得到米非司酮。和路线1相比,仅在环氧化和引入丙炔基的先后顺序上不同,反应步骤相同。总收率35%-40%。
米非司酮文献
J. Reprod. Dev. 61(1) , 67-73, (2015)
The corpus luteum (CL) forms after ovulation and acts as a temporary endocrine gland that produces progesterone (P4), a hormone that is essential for implantation and maintenance of pregnancy in mamma...
Disturbances in production of progesterone and their implications in plant studies.Steroids 96 , 153-63, (2015)
Progesterone is a mammalian hormone that has also been discovered in plants but its physiological function in plants is not explained. Experiments using inhibitors of progesterone synthesis and bindin...
Stress-Immune-Growth Interactions: Cortisol Modulates Suppressors of Cytokine Signaling and JAK/STAT Pathway in Rainbow Trout Liver.PLoS ONE 10 , e0129299, (2015)
Chronic stress is a major factor in the poor growth and immune performance of salmonids in aquaculture. However, the molecular mechanisms linking stress effects to growth and immune dysfunction is poo...
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¥328.0/1g
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产品详情:米非司酮
公司名:上海源溪生物科技有限公司
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相关化合物
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标题:米非司酮_MSDS_用途_密度_米非司酮CAS号【84371-65-3】_化源网 地址:https://m.chemsrc.com/mip/cas/84371-65-3_1150773.html