产品说明书
Estradiol
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同义名 : | 雌二醇 ;β-Estradiol;E2;Dihydrofolliculin;Estrace;Oestradiol;17beta-Estradiol;Beta-Estradiol;17β-Estradiol (CRM);17β-Oestradiol;17β-Estradiol |
| CAS号 : | 50-28-2 | |
| 货号 : | A805521 | |
| 分子式 : | C18H24O2 | |
| 纯度 : | 98+% | |
| 分子量 : | 272.382 | |
| MDL号 : | MFCD00003693 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 60 mg/mL(220.28 mM)，配合低频超声，并水浴加热至45℃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 无水乙醇: 20 mg/mL(73.43 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇 |
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| 动物实验配方： |
IP 2% DMSO+2% Tween80+40% PEG300+water 6 mg/mL clear PO 0.5% CMC-Na 70 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 靶点 |
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| 描述 | ER (Estrogen Receptor) is the receptor of estrogens. 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]. GPR30 (G Protein-Coupled Receptor 30) is a multi-pass membrane protein that localizes to the endoplasmic reticulum. This receptor also binds estrogen and activates multiple downstream signaling pathways. GPR30 plays a role in the rapid nongenomic signaling events widely observed following stimulation of cells and tissues with estrogen. This receptor has been shown to play a role in diverse biological processes[4]. Estradiol is an estrogen that could bind to ER and GPR30. The EC50 reflecting the affinity of estradiol to recombinant human ER was 4×10-8[5]. The growth stimulating EC50 of estradiol on MCF-7 cells was 1.52 μM[6]. Mice were injected intraperitoneally with 100 μl of solution containing 2.5 μg/ml estradiol. Estradiol treatment increased Ki67 staining and mitosis marker phosphor ser10 histone H3 in the uterine epithelial. When estradiol was administrated daily for 3 days, significant increase in uterine weight compared to control group was discovered on the 4th day[7]. In a model of ovariectomized rats, estradiol was subcutaneously injected 2 times at the dose of 10 μg. 2 days following estradiol injection, identical increase in spine density was observed in estradiol-treated mice compared to the control group[8]. | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| AH109 cells | Function assay | 24 h | Agonist activity at ERalpha receptor LBD expressed in yeast AH109 cells assessed as interaction with SRC1 after 24 hrs by alpha-galactosidase assay, EC50=1.05 nM | 22647217 | |
| CHO-K1 cells | Function assay | 24 h | Transcriptional activation of ERbeta receptor expressed in CHO-K1 cells after 24 hrs by luciferase reporter gene assay, EC50=3.6e-05 μM | 22647217 | |
| COS-1 cells | Function assay | In vitro agonist activity for estrogen receptor alpha expressed in COS-1 cells, EC50=2.4 nM | 15713407 | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.67mL 0.73mL 0.37mL |
18.36mL 3.67mL 1.84mL |
36.71mL 7.34mL 3.67mL |
| 参考文献 |
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