产品说明书
Estriol
 |
同义名 : | Oestriol;E3;1,3,5(10)-Estratriene-3,16α,17β-triol;16α-hydroxy-17β-estradiol;Estriol (CRM);NSC-12169 |
| CAS号 : | 50-27-1 | |
| 货号 : | A864579 | |
| 分子式 : | C18H24O3 | |
| 纯度 : | 98+% | |
| 分子量 : | 288.381 | |
| MDL号 : | MFCD00003691 | |
| 存储条件： |
粉末 Keep in dark place,Sealed in dry,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
|
| 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 |
| 生物活性 | |||
|---|---|---|---|
| 靶点 |
|
||
| 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]. | ||
| 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 << | |
| 实验方案 | |||
|---|---|---|---|
| 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 |
| 参考文献 |
|---|