度他雄胺

中文名	度他雄胺
英文名	dutasteride
英文别名	更多

描述

Dutasteride (GG745)是5α还原酶同工酶抑制剂，还可能因其结构域DHT相似对雄激素受体（AR）产生脱靶效应。

相关类别

信号通路 >>

代谢酶/蛋白酶 >>

5 alpha还原酶

研究领域 >>

癌症

溶解度

体外：

DMSO：33.33 mg / mL（63.06 mM;需要超声波）

体内：1。逐个添加每种溶剂：10％DMSO 90％玉米油溶解度：≥2.5mg / mL（4.73 mM）;明确解决方案

储备液

1 mM	1.8920 mL	9.4602 mL	18.9204 mL
5 mM	0.3784 mL	1.8920 mL	3.7841 mL
10 mM	0.1892 mL	0.9460 mL	1.8920 mL

存储

粉末	-20℃下	3年
	4℃下	2年
在溶剂中	-80℃下	6个月
	-20℃下	1个月

运输

室温;可能会有所不同

SMILES

O=C([C@H]1CC[C@]2([H])[C@]1(C)CC[C@]3([H])[C@@]4(C)C=CC(N[C@]4([H])CC[C@]32[H])=O)NC5=CC(C(F)(F)F)=CC=C5C(F)(F)F

参考文献

[1]. Lazier CB, et al. Dutasteride, the dual 5alpha-reductase inhibitor, inhibits androgen action and promotes cell death in the LNCaP prostate cancer cell line. Prostate. 2004 Feb 1;58(2):130-44.

[2]. Biancolella M, et al. Effects of dutasteride on the expression of genes related to androgen metabolism and related pathway in human prostate cancer cell lines. Invest New Drugs. 2007 Oct;25(5):491-7.

[3]. Bramson HN, et al. Unique preclinical characteristics of GG745, a potent dual inhibitor of 5AR. J Pharmacol Exp Ther. 1997 Sep;282(3):1496-502.

[4]. Andriole GL, et al. Clinical usefulness of serum prostate specific antigen for the detection of prostate cancer is preserved in men receiving the dual 5alpha-reductase inhibitor dutasteride. J Urol. 2006 May;175(5):1657-62.

[5]. Margiotta-Casaluci L, et al. Mode of action of human pharmaceuticals in fish: the effects of the 5-alpha-reductase inhibitor, dutasteride, on reproduction as a case study. Aquat Toxicol. 2013 Mar 15;128-129:113-23.

相关活性
小分子

非那雄胺

|

爱普列特

|

CGP-53153

密度	1.3±0.1 g/cm3
沸点	620.3±55.0 °C at 760 mmHg
熔点	242-250?C
分子式	C₂₇H₃₀F₆N₂O₂
分子量	528.530
闪点	329.0±31.5 °C
精确质量	528.221130
PSA	58.20000
LogP	5.61
外观性状	白色结晶固体
蒸汽压	0.0±1.8 mmHg at 25°C
折射率	1.523
储存条件	-20°C Freezer
水溶解性	DMSO: soluble2mg/mL, clear

危险品运输编码	NONH for all modes of transport
海关编码	2942000000

海关编码	2933990090
中文概述	2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%
申报要素	品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期
Summary	2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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…

Preparation of microcapsules with the evaluation of physicochemical properties and molecular interaction.

Arch. Pharm. Res. 37(12) , 1570-7, (2014)

The objective of this study was to prepare and characterize dutasteride (a hydrophobic model drug) microcapsules using ethyl cellulose as a capsule shell polymer with different drug/polymer ratios of …

Long term effectiveness on prescribing of two multifaceted educational interventions: results of two large scale randomized cluster trials.

PLoS ONE 9(10) , e109915, (2014)

Information on benefits and risks of drugs is a key element affecting doctors’ prescribing decisions. Outreach visits promoting independent information have proved moderately effective in changing pre…

(5a,17b)-N-(2,5-Bis(trifluoromethyl)phenyl)-3-oxo-4-azaandrost-1-ene-17-carboxamide

(5α,17β)-N-(2,5-Bis(trifluoromethyl)phenyl)-3-oxo-4-azaandrost-1-ene-17-carboxamide

Avodart

Duagen

α,α,α,α’,α’,α’-Hexafluoro-3-oxo-4-aza-5α-androst-1-ene-17β-carboxy-2′,5′-xylidide

Dutasteride

(4aR,4bS,6aS,7S,9aS,9bS,11aR)-N-[2,5-Bis(trifluoromethyl)phenyl]-4a,6a-dimethyl-2-oxo-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-1H-indeno[5,4-f]quinoline-7-carboxamide

1H-Indeno[5,4-f]quinoline-7-carboxamide, N-[2,5-bis(trifluoromethyl)phenyl]-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-4a,6a-dimethyl-2-oxo-, (4aR,4bS,6aS,7S,9aS,9bS,11aR)-

a,a,a,a’,a’,a’-Hexafluoro-3-oxo-4-aza-5a-androst-1-ene-17b-carboxy-2′,5′-xylidide

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