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Dutasteride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Dutasteride图片
CAS NO:164656-23-9
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
度他雄胺
GG 745
GI 198745
产品介绍
Dutasteride (GG745)是5α 还原酶同工酶 (5α-reductase isozymes) 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。
生物活性

Dutasteride (GG745) is a potent inhibitor of both5α-reductase isozymes. Dutasteride may possess off-target effects on theandrogen receptor(AR) due to its structural similarity to DHT[1].

IC50& Target

IC50: 5 alpha-reductase[1]

体外研究
(In Vitro)

Dutasteride inhibits3H-T conversion to3H-DHT and, as anticipated, inhibits T-induced secretion of PSA and proliferation. However the drug also inhibited DHT-induced PSA secretion and cell proliferation (IC50approximately 1 μM)[1].
Dutasteride competes for binding the LNCaP cell AR with an IC50approximately 1.5 μM. High concentrations of dutasteride (10-50 μM), but not finasteride, in steroid-free medium, resulted in enhanced cell death, possibly by apoptosis[1].
Dutasteride reduces cell viability and cell proliferation in both cell lines tested (androgen-responsive (LNCaP) and androgen-unresponsive (DU145) human prostate cancer (PCa))[2].

体内研究
(In Vivo)

GG745 has a terminal half-life of approximately 240 hr, and single doses of >10 mg decreased DHT levels significantly more than did single 5-mg doses of finasteride[3].
In placebo treated men without prostate cancer there was an 8.3% median increase in PSA at month 24 compared with -59.5% in those who received dutasteride, using doubled values to correct for dutasteride treatment[4].
Toxicity: Dutasteride may affect male fertility and steroid hormone dynamics. Therefore, a 21-day reproduction study was conducted to determine the effects of dutasteride (10, 32 and 100 μg/L) on fish reproduction. Exposure to dutasteride significantly reduced fecundity of fish and affected several aspects of reproductive endocrine functions in both males and females[5].

Clinical Trial
分子量

528.53

性状

Solid

Formula

C27H30F6N2O2

CAS 号

164656-23-9

中文名称

度他雄胺

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 33.33 mg/mL(63.06 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.8920 mL9.4602 mL18.9204 mL
5 mM0.3784 mL1.8920 mL3.7841 mL
10 mM0.1892 mL0.9460 mL1.8920 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (4.73 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.73 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。