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/ Estriol

雌三醇 /Estriol {[allProObj[0].p_purity_real_show]}

货号：A864579 同义名： Oestriol;E3

Estriol is G-protein coupled estrogen receptor antagonist in estrogen receptor-negative breast cancer cells. It is a major urinary estrogen which is largely produced by the placenta during pregnancy.

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
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Estriol 化学结构 CAS号：50-27-1
Estriol 化学结构
CAS号：50-27-1
Estriol 3D分子结构
CAS号：50-27-1
Estriol 化学结构 CAS号：50-27-1
Estriol 3D分子结构 CAS号：50-27-1
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Estriol 纯度/质量文件 产品仅供科研

货号：A864579 标准纯度： {[allProObj[0].p_purity_real_show]}
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Estriol 生物活性

靶点

  • Estrogen receptor
描述 ER (Estrogen Receptor) is the receptor of estrogens. ER is a nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Ligand-dependent nuclear transactivation involves either direct homodimer binding to a palindromic estrogen response element (ERE) sequence or association with other DNA-binding transcription factors to mediate ERE-independent signaling[3].Estriol is an estrogen that could bind to ER and act as a weak ER agonist. However, reports suggested that if in present with estradiol, another stronger ER agonist, estriol acted more like an antagonist[4]. According to data obtained by ligand-binding assay, the affinity of estriol to recombinant human ER was about 10-fold lower than estradiol, as reflected by EC50 values of 2.5×10-7 and 4×10-8, respectively. Estriol could also bind GPR30, as indicated by docking assays and competitive binding assays in ER-negative SKBR3 cells. In a MTT assay, 1 μM estriol prevented SKBR3 cell proliferation induced by 100 nM G-1[5]. Mice were injected intraperitoneally with 100 μl of solution containing 2.5 μg/ml estriol. Estriol treatment increased Ki67 staining and mitosis marker phosphor ser10 histone H3 in the uterine epithelial. When estriol was administrated daily for 3 days, significant increase in uterine weight compared to control group was discovered on the 4th day[6]. Estriol was administrated at the dose of 4 μg/g/day from the first to fifth day after birth to female pups of mPTEN+/- mice. When mice were sacrificed at 52-week-old, none of the 8 mice treated by estriol developed adenocarcinoma, while 3 of the 8 mice in vehicle group developed adenocarcinoma, suggesting estriol suppressed carcinogenesis in this mice model[7].

Estriol 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03617458 Pulmonary Artery Hypertension Phase 2 Recruiting December 2022 United States, Tennessee ... 展开 >> Vanderbilt University Medical Center Recruiting Nashville, Tennessee, United States, 37232 收起 <<
NCT00438464 Adenocarcinoma of the Prostate... 展开 >> Stage II Prostate Cancer 收起 << Phase 2 Completed - United States, Ohio ... 展开 >> Cleveland Clinic Foundation Cleveland, Ohio, United States, 44195 Cleveland Clinic Taussig Cancer Institute, Case Comprehensive Cancer Center Cleveland, Ohio, United States, 44195 United States, Texas University of Texas Southwestern Medical Center Dallas, Texas, United States, 75390 M D Anderson Cancer Center Houston, Texas, United States, 77030 Audie L Murphy Veterans Affairs Hospital San Antonio, Texas, United States, 78209 Cancer Therapy and Research Center San Antonio, Texas, United States, 78229 University Hospital San Antonio, Texas, United States, 78229 University of Texas Health Science Center at San Antonio San Antonio, Texas, United States, 78229 收起 <<
NCT01009723 - Unknown July 2012 United States, Massachusetts ... 展开 >> Integrated Genetics Westborough, Massachusetts, United States, 01581 United States, New Mexico Integrated Genetics Santa Fe, New Mexico, United States, 87505 收起 <<

Estriol 参考文献

[1]Lappano R, Rosano C, et al. Estriol acts as a GPR30 antagonist in estrogen receptor-negative breast cancer cells. Mol Cell Endocrinol. 2010 May 14;320(1-2):162-70.

[2]Melamed M, Castano E, et al. Molecular and kinetic basis for the mixed agonist/antagonist activity of estriol. Mol Endocrinol. 1997 Nov;11(12):1868-78.

[3]Saville B, Wormke M, Wang F, Nguyen T, Enmark E, Kuiper G, Gustafsson JA, Safe S. Ligand-, cell-, and estrogen receptor subtype (alpha/beta)-dependent activation at GC-rich (Sp1) promoter elements. J Biol Chem. 2000 Feb 25;275(8):5379-87.

[4]Melamed M, Castaño E, Notides AC, Sasson S. Molecular and kinetic basis for the mixed agonist/antagonist activity of estriol. Mol Endocrinol. 1997 Nov;11(12):1868-78.

[5]Lappano R, Rosano C, De Marco P, De Francesco EM, Pezzi V, Maggiolini M. Estriol acts as a GPR30 antagonist in estrogen receptor-negative breast cancer cells. Mol Cell Endocrinol. 2010 May 14;320(1-2):162-70.

[6]Hewitt SC, Korach KS. Estrogenic activity of bisphenol A and 2,2-bis(p-hydroxyphenyl)-1,1,1-trichloroethane (HPTE) demonstrated in mouse uterine gene profiles. Environ Health Perspect. 2011 Jan;119(1):63-70.

[7]Begum M, Tashiro H, Katabuchi H, Suzuki A, Kurman RJ, Okamura H. Neonatal estrogenic exposure suppresses PTEN-related endometrial carcinogenesis in recombinant mice. Lab Invest. 2006 Mar;86(3):286-96.

Estriol 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.47mL

0.69mL

0.35mL

17.34mL

3.47mL

1.73mL

34.68mL

6.94mL

3.47mL

Estriol 技术信息

CAS号50-27-1
分子式C18H24O3
分子量 288.381
别名 Oestriol;E3;1,3,5(10)-Estratriene-3,16α,17β-triol;16α-hydroxy-17β-estradiol;Estriol (CRM);NSC-12169
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,Room Temperature
溶解度

DMSO: 250 mg/mL(866.91 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 9 mg/mL clear

PO 0.5% CMC-Na 50 mg/mL suspension

Tags: Estriol | Oestriol;E3;1,3,5(10)-Estratriene-3,16α,17β-triol;16α-hydroxy-17β-estradiol;Estriol (CRM);NSC-12169 | Estrogen | ERR | AmBeed-信号通路专用抑制剂 | Estriol 纯度/质量文件 | Estriol 生物活性 | Estriol 临床数据 | Estriol 参考文献 | Estriol 实验方案 | Estriol 技术信息

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