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屈洛昔芬

屈洛昔芬用途

Droloxifene,Tamoxifen 衍生物,是一种具有口服活性和选择性的雌激素受体 (estrogen receptor) 调节剂。Droloxifene 具有抗雌激素和抗植入作用。Droloxifene 诱导 MCF-7 细胞 p53 表达及凋亡。Droloxifene 预防去卵巢大鼠骨丢失。

屈洛昔芬名称

[ CAS 号 ]:
82413-20-5

[ 中文名 ]:
屈洛昔芬

[ 英文名 ]:
Droloxifene

[中文别名 ]:

[英文别名 ]:

屈洛昔芬生物活性

[ 描述 ]:

Droloxifene,Tamoxifen 衍生物,是一种具有口服活性和选择性的雌激素受体 (estrogen receptor) 调节剂。Droloxifene 具有抗雌激素和抗植入作用。Droloxifene 诱导 MCF-7 细胞 p53 表达及凋亡。Droloxifene 预防去卵巢大鼠骨丢失。

[ 相关类别 ]:

信号通路 >> 其他 >> 雌激素受体/ERR
研究领域 >> 癌症

[体外研究]

Droloxifene(10nm；16-18h)诱导MCF-7细胞凋亡[1]。细胞活力测定[2]细胞株：MCF-7细胞浓度：10nm培养时间：16-18h结果：诱导细胞凋亡

[体内研究]

屈洛昔芬(5-20 mg/kg；p.o.；每日4周)以10 mg/kg的剂量增加DFM的骨密度,并完全防止20 mg/kg/天的剂量降低去卵巢(OVX)引起的DFM的骨密度和骨密度[3]。动物模型：5月龄假手术大鼠[3]剂量：5、10、20 mg/kg口服；每日4周结果：10 mg/kg时DFM的骨密度显著增加；20 mg/kg/d时完全阻止OVX所致DFM的骨密度和骨密度下降。

[参考文献]

[1]. Herrington DM, et al. Cardiovascular effects of droloxifene, a new selective estrogen receptor modulator, in healthypostmenopausal women. Arterioscler Thromb Vasc Biol. 2000 Jun;20(6):1606-12.

[2]. Grasser WA, et al. Common mechanism for the estrogen agonist and antagonist activities of droloxifene. J Cell Biochem. 1997 May;65(2):159-71.

[3]. Ke HZ, et al. Droloxifene, a new estrogen antagonist/agonist, prevents bone loss in ovariectomized rats. ndocrinology. 1995 Jun;136(6):2435-41.

[4]. Huang Y, et al. Anti-implantation effect of droloxifene in rats and its relationship with anti-estrogenic activity. Acta Pharmacol Sin. 2005 Oct;26(10):1243-7.

屈洛昔芬物理化学性质

[ 密度 ]:
1.092 g/cm3

[ 沸点 ]:
526.6ºC at 760 mmHg

[ 熔点 ]:
127-129ºC

[ 分子式 ]:
C26H29NO2

[ 分子量 ]:
579.63700

[ 精确质量 ]:
579.24700

[ PSA ]:
164.83000

[ LogP ]:
4.45320

[ 外观性状 ]:
灰白色至灰白的-米色固体

[ 折射率 ]:
1.596

[ 储存条件 ]:
Amber Vial, -20°C Freezer

屈洛昔芬毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
SL1209900
CHEMICAL NAME :
Phenol, 3-(1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenyl-1-b utenyl)-, (E)-
CAS REGISTRY NUMBER :
82413-20-5
LAST UPDATED :
199704
DATA ITEMS CITED :
7
MOLECULAR FORMULA :
C26-H29-N-O2
MOLECULAR WEIGHT :
387.56

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 :
>4500 mg/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: 9,186,1984
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>2250 mg/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: 9,186,1984
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
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: 9,186,1984
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>1500 mg/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: 9,186,1984 *** REVIEWS *** IARC Cancer Review:Human Inadequate Evidence IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 66,241,1996 IARC Cancer Review:Animal Inadequate Evidence IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 66,241,1996 IARC Cancer Review:Group 3 IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 66,241,1996

屈洛昔芬安全信息

[ 危害码 (欧洲) ]:
Xi

屈洛昔芬合成路线

详细合成路线

屈洛昔芬上下游产品

屈洛昔芬上游产品

屈洛昔芬下游产品

推荐生产厂家/供应商：

公司名：上海源溪生物科技有限公司

区域：上海市浦东新区

价格：
￥需询单/1g

联系人：赖经理

产品详情：Droloxifene

公司名：上海阿拉丁生化科技股份有限公司

区域：上海市浦东新区

价格：
￥810.0/25mg ￥4560.0/100mg ￥需询单/1g ￥需询单/1g

联系人：阿拉丁李高志

产品详情：屈洛昔芬

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