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雄酮

雄酮用途

Androsterone 是睾酮的代谢产物,可以激活法尼醇 X 受体 (FXR)。

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雄酮名称

[ CAS 号 ]:
53-41-8

[ 中文名 ]:
雄酮

[ 英文名 ]:
Androsterone

[中文别名 ]:

酮基化甾醇

[英文别名 ]:

3-α-hydroxy-5α-Androstan-17-one
MFCD01317504
Androkinine
5a-Androsterone
Androkinin
Androtine
3alpha-Hydroxy-5alpha-androstan-17-one
Atromide ICI
3-Epihydroxyetioallocholan-17-one
(3a,5a)-3-Hydroxyandrostan-17-one

雄酮生物活性

[ 描述 ]:

Androsterone 是睾酮的代谢产物,可以激活法尼醇 X 受体 (FXR)。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> FXR

研究领域 >> 代谢疾病

研究领域 >> 神经疾病

天然产物 >> 类固醇

[ 靶点 ]

Human Endogenous Metabolite

[体外研究]

雄激素激活mFXR-LBD和hFXR-LBD,雄激素激活mFXR-LBD的能力强于hFXR-LBD。此外,用gal4-hFXR-LBD和SRC-1/VP16表达质粒进行的共转染研究表明,雄激素增强了SRC-1与hFXR-LBD的相互作用。包括H294S,S332V,R351H和Y361F在内的几种氨基酸变化显着降低了雄激素的活化[1]。雄激素(5α,3α-A)(10至100μM)也在体外切片模型中以浓度依赖性方式抑制癫痫样放电[2]。

[体内研究]

雄激素治疗导致小异二聚体伴侣(SHP)的显着诱导,表明雄激素可能激活内源性FXR [1]。腹腔注射雄甾酮(5α,3α-A)以剂量依赖的方式保护小鼠免受以下模型中的癫痫发作(ED50,剂量以mg/kg保护50％的动物)：6 Hz电刺激(29.1),戊四唑( 43.5),毛果芸香碱(105),4-AP(215)和最大电休克(224)[2]。

[细胞实验]

使用AML-12细胞并在补充有10％胎牛血清，1％胰岛素转铁蛋白 - 硒混合物，40ng / mL地塞米松，100U / mL青霉素的DMEM / Ham's F12培养基的1：1混合物中培养，并且100μg/ mL链霉素。对于基因调控研究，将AML-12细胞以每孔4×10 5个细胞接种在生长培养基中的六孔板中。第二天，向培养基中加入包括雄甾酮或二甲基亚砜（DMSO）载体的处理。在添加处理后的不同时间，制备总RNA。单个基因的mRNA水平通过实时PCR确定[1]。

[动物实验]

在研究开始前2周，将8至10周龄的阉割雄性小鼠喂食酪蛋白饮食2周。小鼠每天皮下注射0.1mL 90％玉米油/ 10％乙醇载体或10mg / mL雄甾酮。在第五次每日治疗后2小时，在光周期开始后约4小时，杀死动物。制备总RNA，并通过实时PCR确定特定基因的mRNA水平[1]。

[参考文献]

[1]. Wang S, et al. The nuclear hormone receptor farnesoid X receptor (FXR) is activated by androsterone. Endocrinology. 2006 Sep;147(9):4025-33.

[2]. Kaminski RM, et al. Anticonvulsant activity of androsterone and etiocholanolone. Epilepsia. 2005 Jun;46(6):819-27.

[相关活性小分子]

雄酮物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
413.1±45.0 °C at 760 mmHg

[ 熔点 ]:
180-185ºC

[ 分子式 ]:
C₁₉H₃₀O₂

[ 分子量 ]:
290.440

[ 闪点 ]:
176.4±21.3 °C

[ 精确质量 ]:
290.224579

[ PSA ]:
37.30000

[ LogP ]:
3.75

[ 外观性状 ]:
白色颗粒

[ 蒸汽压 ]:
0.0±2.2 mmHg at 25°C

[ 折射率 ]:
1.536

[ 储存条件 ]:
室温

雄酮MSDS

详细MSDS(安全技术说明书)

雄酮毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: BV8053000

CHEMICAL NAME :: 5-alpha-Androstan-17-one, 3-alpha-hydroxy-

CAS REGISTRY NUMBER :: 53-41-8

BEILSTEIN REFERENCE NO. :: 2217626

LAST UPDATED :: 199612

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C19-H30-O2

MOLECULAR WEIGHT :: 290.49

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 8400 ug/kg

SEX/DURATION :: male 21 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - testes, epididymis, sperm duct

REFERENCE :: ENDOAO Endocrinology (Baltimore). (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21203) V.1- 1917- Volume(issue)/page/year: 21,313,1937

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 80 mg/kg

SEX/DURATION :: female 13-20 day(s) after conception

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

REFERENCE :: ENDOAO Endocrinology (Baltimore). (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21203) V.1- 1917- Volume(issue)/page/year: 99,1490,1976 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X3818 No. of Facilities: 53 (estimated) No. of Industries: 2 No. of Occupations: 2 No. of Employees: 767 (estimated) No. of Female Employees: 347 (estimated)

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雄酮安全信息

[ 符号 ]:

GHS07, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H315-H319-H334-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338-P342 + P311

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Faceshields;Gloves

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
36/37/38-43

[ 安全声明 (欧洲) ]:
22-24/25

[ 危险品运输编码 ]:
2811.0

[ WGK德国 ]:
3

[ RTECS号 ]:
BV8053000

[ 危险类别 ]:
6.1

雄酮合成路线

详细合成路线

雄酮上下游产品

雄酮上游产品

雄酮下游产品

雄酮文献

Silica-based nanofibers for electrospun ultra-thin layer chromatography.

J. Chromatogr. A. 1364 , 261-70, (2014)

Nanofibrous silica-based stationary phases for electrospun ultra-thin layer chromatography (E-UTLC) are described. Nanofibers were produced by electrospinning a solution of silica nanoparticles disper...

Chemical genetics reveals a complex functional ground state of neural stem cells.

Nat. Chem. Biol. 3(5) , 268-273, (2007)

The identification of self-renewing and multipotent neural stem cells (NSCs) in the mammalian brain holds promise for the treatment of neurological diseases and has yielded new insight into brain canc...

Next-generation steroidogenesis inhibitors, dutasteride and abiraterone, attenuate but still do not eliminate androgen biosynthesis in 22RV1 cells in vitro

J. Steroid Biochem. Mol. Biol. 144 Pt B , 436-44, (2014)

• Dutasteride and abiraterone were evaluated for inhibition of steroidogenesis. • Bypass mechanisms arise in the presence of abiraterone to form DHT. • Dutasteride inhibits T and DHT effectively in vi...

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雄酮