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Estriol作用于雌激素受体阴性乳腺癌细胞，拮抗G-蛋白偶联雌激素受体。
别名：Oestriol
Estriol作用于雌激素受体阴性乳腺癌细胞，拮抗G-蛋白偶联雌激素受体。1 μM Estriol 作用于SkBr3细胞，通过作为GPR30依赖性通路的拮抗剂，而废除100 nM G-1诱导的增殖效果。Estriol 具有抗雌激素活性，通过干扰雌激素诱导的阳性 共同结合和受体二聚化，及hER复合体与 ERE结合,也降低 雌激素依赖性转录，这种作用存在剂量依赖性。最新研究显示雌激素(Estrone, Estradiol, 和Estriol)抑制Alzheimer疾病相关的Aβ低聚物形成，且在体外，Estriol 活性最强。
| 细胞实验 | |
|---|---|
| 细胞系 | SkBr3 cells |
| 方法 | For the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, culturing cells in 96-well plates under 200 μL of growth medium and at an initial density of 10,000 cells per well. Washing cells once they have attached and further incubated in medium which contains 2.5% charcoal-stripped FBS with the indicated treatment. Changing the medium every 2 days (with treatment). Where applicable,transfecting 200 ng of the indicated plasmids every 2 days before treatments using Fugene6 Reagent, as recommended by the manufacturer. Following 6 days of incubation, adding the assay mixture (10µL per well) which contains 1mg/mL 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) to each well and incubated at 37 ◦C for 4 h in a 5% CO2 atmosphere. The yellow tetrazolium MTT, reduced by metabolically active cells, results in intracellular purple formazan, which is released after overnight incubation with 200 µL 1% sodium dodecyl sulfate in 0.01N HCL and quantified spectrophotometrically by reading absorbance at 570nm using an enzyme-linked immunosorbent assay plate reader. |
| 浓度 | ~100 nM |
| 处理时间 | 6 days |
| 动物实验 | |
|---|---|
| 动物模型 | mPTEN+/- and wild-type mice |
| 配制 | Estriol is dissolved in ethanol and corn oil. |
| 剂量 | 4 μg/g/day |
| 给药处理 | Administrated via s.c.SkBr3 细胞 |
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 | |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km 系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量，需要将22.4 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到白藜芦醇用于大鼠的等效剂量为11.2 mg/kg。
| 分子量 | 288.39 |
| 分子式 | C18H24O3 |
| CAS号 | 50-27-1 |
| 纯度 | 99.43% |
| 溶解性（25°C） | DMSO 45 mg/mL |
| 储存和运输条件 |
固体粉末： -20°C 冷藏长期储存
常温运输及临时存放 |
以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.4675 mL | 17.3376 mL | 34.6753 mL |
| 5 mM | 0.6935 mL | 3.4675 mL | 6.9351 mL |
| 10 mM | 0.3468 mL | 1.7338 mL | 3.4675 mL |
Expert Opin Ther Targets. 2020 Apr;24(4):389-402.
Cepharanthine hydrochloride induces mitophagy targeting GPR30 in hepatocellular carcinoma (HCC)
Estriol购买自AbMole
 |
数据来源 | Expert Opinion on Therapeutic Targets 2020 Apr. Figure 4. Estriol (Abmole Bioscience, USA) |
| 方法 | Western blotting | |
| 细胞系 | Huh7 cells | |
| 浓度 | 1 μM | |
| 处理时间 | 12 h | |
| 实验结果 | Furthermore, in Huh7 and HepG2 cells, increased p-DRP1 induced by CH can be reduced by Estriol (E3), which is an inhibitor of GPR30, thus suggesting that CH may play an estrogen-like role in activating the GPR30 signaling cascade in HCC cells. |
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| GDC-0810
GDC-0810 (Brilanestrant, ARN-81) 是一种口服生物可利用的选择性雌激素受体降解剂（SERD），IC50 值为 0.7 nM。 |
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PHTPP is a selective estrogen receptor β (ERβ) full antagonist with 36-fold selectivity for ERβ over ERα. |
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