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CAS No.: 979-32-8

β-Estradiol 17-Valerate/戊酸雌二醇 Catalog No. CSN10936

Synonyms: β-Estradiol 17-valerate;Estradiol Valerianate;Estradiol 17β-valerate

Estradiol Valeate is a synthetic estrogen. Formulations containing estradiol valerate with other steroid hormones have been used to treat endometriosis.

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生物活性

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. 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. Estradiol Valeate is the valeate form of Estradiol. 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. The growth stimulating EC₅₀ of estradiol on MCF-7 cells was 1.52 μM. 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. 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.
参考文献

[1] Takabe K, Kim RH, et al. Estradiol induces export of sphingosine 1-phosphate from breast cancer cells via ABCC1 and ABCG2. J Biol Chem. 2010 Apr 2;285(14):10477-86.
[2] Wickramasinghe NS, Manavalan TT, et al.Estradiol downregulates miR-21 expression and increases miR-21 target gene expression in MCF-7 breast cancer cells. Nucleic Acids Res. 2009 May;37(8):2584-95.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8051 mL
- 14.0253 mL
- 28.0506 mL
- 5 mM
- 0.5610 mL
- 2.8051 mL
- 5.6101 mL
- 10 mM
- 0.2805 mL
- 1.4025 mL
- 2.8051 mL

技术信息

CAS号

979-32-8

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H32O3

运输

蓝冰

分子量

356.50

别名

β-Estradiol 17-valerate;Estradiol Valerianate;Estradiol 17β-valerate;NSC 17590;Altadiol;Deladiol;Delestrogen;Estraval;Progynova;Valergen;oestradiol valerate;17Estradiol17valerate pentanoate destra135(10)trine3ol17yle;戊酸雌二醇

溶解度

DMSO	71.0 mg/mL (199.2 mM)
Water	Insoluble
Ethanol	Insoluble

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