Estradiol Benzoate
(Synonyms: 苯甲酸雌二醇; β-Estradiol 3-benzoate; 17β-Estradiol 3-benzoate) 目录号 : GC15245
Estradiol Benzoate是一种HBx蛋白抑制剂，可抑制雄激素和乙型肝炎病毒(HBV)的转录和复制。Estradiol Benzoate具有抗生育作用、抗弓形虫活性，并能改善卵巢切除(Ovx)雌性小鼠的记忆行为。
Cas No.:50-50-0
Sample solution is provided at 25 µL, 10mM.
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Estradiol Benzoate is a HBx protein inhibitor and inhibits androgen and hepatitis B virus (HBV) transcription, replication. Estradiol Benzoate shows antifertility effects, anti- Toxoplasma gondii activity and can improve memory behavior of Ovariectomy (Ovx) female mice[1][2][3][4].
Estradiol Benzoate (0-500µM; 48h) delays or stops the cell cycle of tachyzoites by blocking progression from G1 to S phase in HFF cells[1]. Estradiol Benzoate (35-75µM; 2d) significantly reduced the production of HBeAg, HBsAg, HBV pgRNA, and HBV DNA in HepG2 cells in a dose-dependent manner and inhibited HBV activity[2].
After male mice were exposed to Estradiol Benzoate (5, 10mg/kg, SC), as the concentration of Estradiol Benzoate increased, the number of TUNEL-positive cells in the testes of Estradiol Benzoate-treated mice significantly increased, and pro-apoptotic factors (Fas, TNF, Cytochrome C , Apaf1, Chop, Caspase-3, Caspase-8, Caspase-9 and Caspase-12) and estrogen receptor (ER) signaling pathway key genes (ER α, ER β, Erk1/2, Hsp90 and DAX-1) The mRNA expression level of was significantly up-regulated in the testis of the treatment group[3]. In an ovariectomy model, Estradiol Benzoate (20-200µg/kg for 4-5weeks) effectively normalised ovariectomy-induced changes in female rats, including a reduction in the width of the synaptic gap, an expansion in the thickness of the postsynaptic dense substance (PSD) and an increase in the number of presynaptic mid-synaptic vesicles in the Fr1 and hippocampal CA1 regions of the cerebral cortex[4].
References:
[1]. Lu D, Zhang N Z, Yao Y, et al. Investigation of antiparasitic activity of two marine natural products, estradiol benzoate, and octyl gallate, on Toxoplasma gondii in vitro[J]. Frontiers in Pharmacology, 2022, 13: 841941.
[2]. He J, Wu J, Chen J, et al. Identification of estradiol benzoate as an inhibitor of HBx using inducible stably transfected HepG2 cells expressing HiBiT tagged HBx[J]. Molecules, 2022, 27(15): 5000.
[3]. Lei X, Cui K, Liu Q, et al. Exogenous estradiol benzoate induces spermatogenesis disorder through influencing apoptosis and oestrogen receptor signalling pathway[J]. Reproduction in domestic animals, 2016, 51(1): 75-84.
[4]. Xu X, Zhang Z. Effects of estradiol benzoate on learning-memory behavior and synaptic structure in ovariectomized mice[J]. Life sciences, 2006, 79(16): 1553-1560.
Estradiol Benzoate是一种HBx蛋白抑制剂，可抑制雄激素和乙型肝炎病毒(HBV)的转录和复制。Estradiol Benzoate具有抗生育作用、抗弓形虫活性，并能改善卵巢切除(Ovx)雌性小鼠的记忆行为[1][2][3][4]。
Estradiol Benzoate（0-500µM；48h）通过阻断HFF细胞从G1期到S期的进展来延迟或停止弓形虫速殖子的细胞周期[1]。Estradiol Benzoate（35-75µM；2d）以剂量依赖性的方式显著降低HepG2 细胞中HBeAg、HBsAg、HBV pgRNA和HBV DNA的产生，并抑制 HBV活性[2]。
雄性小鼠暴露于Estradiol Benzoate（5、10mg/kg）后，随着Estradiol Benzoate浓度的增加，Estradiol Benzoate组小鼠睾丸中TUNEL阳性细胞数显著增加，促凋亡因子(Fas、TNF、细胞色素C、Apaf1、Chop、Caspase-3、Caspase-8、Caspase-9和Caspase-12)和雌激素受体(ER)信号通路关键基因(ERα、ERβ、Erk1/2、Hsp90和DAX-1)的mRNA表达水显著上调[3]。在卵巢切除模型中，Estradiol Benzoate（20-200µg/kg，4-5weeks）有效地使雌性大鼠卵巢切除引起的变化正常化，包括减少突触间隙的宽度，扩大突触后致密物（PSD）的厚度，并增加大脑皮层Fr1和海马CA1区突触前中突触小泡的数量[4]。
| Cell experiment [1]: | |
Cell lines | HepG2 cells |
Preparation Method | HepG2 cells were plated in 12-well plates. Then, Estradiol Benzoate were added at final concentrations of 35µM, 55µM, and 75µM for two days, while 1% DMSO DMEM was used as the control group. |
Reaction Conditions | 35, 55, 75µM; 2d |
Applications | Estradiol Benzoate significantly reduced the production of HBeAg, HBsAg, HBV pgRNA, and HBV DNA in a dose-dependent manner and inhibited HBV activity. |
| Animal experiment [2]: | |
Animal models | Ovariectomy (Ovx) |
Preparation Method | One week after ovariectomy (Ovx), ICR female mice received daily injection of Estradiol Benzoate (20, 100, 200µg/kg; sc) for 4-5 weeks. Spatial memory was then tested in the water maze, and the overall locomotor activity was monitored in open field. |
Dosage form | 20, 100, 200µg/kg; sc; 4-5 weeks |
Applications | Estradiol Benzoate replacement effectively normalized the changes induced by Ovx, reducing the width of the synaptic cleft, enlarging the thickness of postsynaptic density (PSD), and increasing the number of synaptic vesicles in the presynapse in both cerebral cortex Fr1 and hippocampus CA1 areas. |
References: | |
| Cas No. | 50-50-0 | SDF | |
| 别名 | 苯甲酸雌二醇; β-Estradiol 3-benzoate; 17β-Estradiol 3-benzoate | ||
| 化学名 | [(8R,9S,13S,14S,17S)-17-hydroxy-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-3-yl] benzoate | ||
| Canonical SMILES | CC12CCC3C(C1CCC2O)CCC4=C3C=CC(=C4)OC(=O)C5=CC=CC=C5 | ||
| 分子式 | C25H28O3 | 分子量 | 376.49 |
| 溶解度 | ≥ 12.15mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6561 mL | 13.2806 mL | 26.5611 mL |
| 5 mM | 0.5312 mL | 2.6561 mL | 5.3122 mL |
| 10 mM | 0.2656 mL | 1.3281 mL | 2.6561 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >99.50%
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