Droloxifene(Synonyms: 3-Hydroxytamoxifen)

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Droloxifene (Synonyms: 3-Hydroxytamoxifen) 纯度: 99.68%

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。

Droloxifene(Synonyms: 3-Hydroxytamoxifen)

Droloxifene Chemical Structure

CAS No. : 82413-20-5

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5 mg ￥2500 In-stock
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Droloxifene 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Anti-Cancer Compound Library

生物活性

Droloxifene, a Tamoxifen derivative, is an orally active and selective estrogen receptor modulator. Droloxifene shows antiestrogenic and anti-implantation effects. Droloxifene induces p53 expression and apoptosis in MCF-7 cells. Droloxifene prevents bone loss in ovariectomized rats [1][2][3].

体外研究
(In Vitro)

Droloxifene (10 nM; 16-18 hours) induces apoptosis in MCF-7 cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: MCF-7 cells
Concentration: 10 nM
Incubation Time: 16-18 hours
Result: Induced cells apoptosis

体内研究
(In Vivo)

Droloxifene (5-20 mg/kg; p.o.; daily for 4 weeks) increases BMD of DFM at 10mg/kg, and completely prevents the decrease of BMC and BMD of DFM induced by ovariectomized (OVX) at 20 mg/kg/day[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 5-month-old sham-operate rats[3]
Dosage: 5, 10, 20 mg/kg
Administration: Oral; daily for 4 weeks
Result: BMD of DFM increased significantly at 10mg/kg; completely prevented the decrease of BMC and BMD of DFM induced by OVX at 20 mg/kg/day.

分子量

387.51

Formula

C26H29NO2
CAS 号

82413-20-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (129.03 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5806 mL 12.9029 mL 25.8058 mL
5 mM 0.5161 mL 2.5806 mL 5.1612 mL
10 mM 0.2581 mL 1.2903 mL 2.5806 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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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: ≥ 5 mg/mL (12.90 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (12.90 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 50.0 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 上海金畔生物科技有限公司 网站选购。
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.

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