Estriol是一种具有口服活性的雌激素,是 ERα 和 ERβ 激动剂。Estriol 在雌激素受体阴性乳腺癌细胞中是有效的 GPR30 拮抗剂。Estriol 可以通过减少组织炎症的免疫调节机制来减轻疾病的严重程度。
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 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
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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]. |
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 << | |
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 |
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 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place,Sealed in dry,Room Temperature |
溶解方案 |
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 以下溶解方案都请先按照体外实验的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
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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 |