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Mestranol
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很棒纯度: 99.16%
货号 T1579Cas号 72-33-3
别名 美雌醇, Norquen, Menophase, Devocin
Mestranol (Devocin) 是一种雌激素受体激动剂，是一种非活性的前药，在转化为炔雌醇时具有生物活性。动物实验中，它可以与黄体酮联合使用，它可用于更年期激素或月经紊乱的研究。
其他形式的 “Mestranol”:
Mestranol
一键复制产品信息 很棒纯度: 99.16%
货号 T1579 别名 美雌醇, Norquen, Menophase, DevocinCas号 72-33-3
Mestranol (Devocin) 是一种雌激素受体激动剂，是一种非活性的前药，在转化为炔雌醇时具有生物活性。动物实验中，它可以与黄体酮联合使用，它可用于更年期激素或月经紊乱的研究。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 25 mg | ¥ 279 | 现货 | |
| 50 mg | ¥ 398 | 现货 | |
| 100 mg | ¥ 578 | 现货 | |
| 200 mg | ¥ 849 | 现货 | |
| 500 mg | ¥ 1,420 | 现货 | |
| 1 mL x 10 mM (in DMSO) | ¥ 297 | 现货 |
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产品介绍
Mestranol AI Summary
Mestranol exhibits a high oral antifertility potency in rats, exceeding that of ethynylestradiol at doses greater than 2.0 mg/kg/day, and demonstrates lower oral estrogenic potency than ethynylestradiol at 0.3 mg/kg/day. It shows oral estrogenic activity in uterotropic assays in rats at doses ranging from 100 to 10,000 ng, causing a decrease in weight by 65.3 mg. Mestranol is involved in diverse biological activities, including modulation of Lamin A splicing, mitochondrial fusion, and inhibition of ROR gamma, GCN5L2, and human tyrosyl-DNA phosphodiesterase 1 among others. It also inhibits chronic active B-cell receptor signaling, malarial parasite plastid function, and HP1-beta chromodomain interactions, and corrects the CFTR Delta508 mutation and blocks Ebola virus entry.
In radioligand binding assays, Mestranol shows moderate potency in inhibiting the Norepinephrine Transporter and higher affinity for the Estrogen ERalpha receptor, while displaying weaker interactions with other receptors such as Cannabinoid CB1 and Progesterone receptors. It also exhibits inhibitory effects on the Serotonin transporter and moderate potency against the Sodium Channel, Site 2. Moreover, this compound has shown potent inhibition of the human CYP3A4 enzyme system.
In anti-viral assays, Mestranol demonstrates inhibition of SARS-CoV-2 induced cytotoxicity in Vero E6 and Caco-2 cells, and inhibition of SARS-CoV-2 3CL-Pro protease activity. It also exhibits antifungal activity against Candida albicans and some antibacterial activities against various bacterial strains including Klebsiella pneumoniae and Pseudomonas aeruginosa. Additionally, it shows antiproliferative activity against human MCF7 cells with an IC50 value of 40.0 nM.
In FDA HLAED assays, it shows varied liver enzyme activity, indicating potential effects on liver function. Mestranol also participates in numerous physiological processes as suggested by bioactivity in assays related to liver and kidney functions, electrolyte balance, and hematologic parameters. Overall, Mestranol presents a broad spectrum of bioactivities, making it a significant candidate for further biomedical research across multiple therapeutic areas..
Note: Summary generated by AI. Data source: ChEMBL 
生物活性
化学信息
储存&溶解度
| 产品描述 | Mestranol (Devocin), a semisynthetic estrogen, is used as an estrogen receptor agonist and must be demethylated to be biologically active. |
| 体外活性 | 在大鼠中,Mestranol（0.2 mg / kg）能够增加由表达AHF的谷胱甘肽S-转移酶（PGST）占据的肝脏的比例. 口服Mestranol（0.02 mg / kg和0.2 mg / kg）增加局灶性肝细胞标记指数.在大鼠额叶皮层和孤束核（NTS）中,Mestranol（50 mg / 100 g b.wt.）能够使α-2肾上腺素能受体明显减少. |
| 体内活性 | Mestranol 能够作用于雌激素受体（ER）,并被代谢为羟基化产物。 |
| 别名 | 美雌醇, Norquen, Menophase, Devocin |
| 分子量 | 310.43 |
| 分子式 | C21H26O2 |
| CAS No. | 72-33-3 |
| Smiles | COC1=CC2=C(C=C1)C1CCC3(C)C(CCC3(O)C#C)C1CC2 |
| 密度 | 1.0865 g/cm3 (Estimated) |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 12 mg/mL (38.66 mM), Sonication is recommended.  H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 24 mg/mL (77.31 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
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DMSO/Ethanol
Ethanol
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计算器
体内实验配液计算器
请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：
比如您的给药剂量是10 mg/kg，每只动物体重20g，给药体积100 μL， 一共给药动物10只，您使用的配方为5%
DMSO + 30%PEG300 + 5%Tween 80 + 60%Saline/PBS/ddH2O， 那么您的工作液浓度为2mg/mL。 以上为“体内实验配液计算器”的使用方法举例，并不是具体某个化合物的推荐配制方式，请根据您的实验动物和给药方式选择适当的溶解方案。
剂量转换
对于不同动物的给药剂量换算，您也可以参考 更多
预览
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