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Gestrinone研究進展

發(fā)布日期：2017-10-30   瀏覽次數：0
核心提示：a href=https://www.medchemexpress.com/Gestrinone.htmlGestrinone/a產品描述：Gestrinone (R2323) is a synthetic steroid hor
<a href="https://www.medchemexpress.com/Gestrinone.html">Gestrinone</a>產品描述：Gestrinone (R2323) is a synthetic steroid hormone used to treat endometriosis. It inhibits leiomyoma cells with an <b>IC<sub>50</sub></b> of 43.67 μM.

IC50 & Target: IC50: 43.67 μM (leiomyoma cells)<sup>[2]</sup>

<i><b>In Vitro:</b></i> Gestrinone binds to endometrial receptors for estrogen, progesterone and androgen, occupies all specific binding sites of steroids in the steroid target cells despite the presence of endogenous steroids<sup>[1]</sup>. Gestrinone exhibits stronger inhibitory effects on the growth of leiomyoma cells at 60 h than that at 20 and 40 h. Leiomyoma cells appears less dense, the cytoplasm is atrophic, the intercellular connections dwindled and nuclear aggregations are observed with more than 10 μM gestrinone treatment. Gestrinone treatment reduces the relative mRNA levels of estrogen α in a concentration dependent manner at concentrations of 0.1-3.0 μM<sup>[2]</sup>.

<i><b>In Vivo:</b></i> The estrogen-sensitive endpoints, vaginal keratinization and uterine <br><br>
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