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产品描述： Nestoron, a synthetic progestin, is a high-affinity agonist of the progesterone receptor (EC50: 10.3 nM). |
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靶点：
Estrogen/progestogen Receptor;Progesterone Receptor;Estrogen/progestogenReceptor |
体内研究：
The potency of Nestorone was over 100-fold higher upon s.c. administration than via the oral route. Nestorone showed no androgenic or anabolic activity. Nestorone did not bind to sex hormone binding globulin (SHBG). In contrast to estradiol and levonorgestrel, Nestorone showed no uterotropic activity in ovariectomized rats. Despite significant binding to glucocorticoid receptors (GR), Nestorone showed no glucocorticoid activity in vivo |
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动物实验：
Immature female rats were ovariectomized under methoxylflurane anesthesia, randomly distributed into treatment groups (n 5 6 per group), and used 5 to 7 days later. Levonorgestrel or Nestorone (1 or 5 mg) was injected s.c. daily for 5 days. Vaginal lavages were examined microscopically to detect vaginal cornification. The animals were killed on day 6, and the uteri were removed, cleaned, blotted dry, and weighed. The antiestrogenic effects of levonorgestrel and Nestorone were determined in rats receiving 1.0 mg E2. A positive control group received E2 alone. Negative controls received the vehicle |
参考文献：
1.Kumar N, et al. Nestorone: a progestin with a unique pharmacological profile. Steroids. 2000 Oct-Nov;65(10-11):629-36. 2.Chen S, et al. Therapeutic progestin segesterone acetate promotes neurogenesis: implications for sustaining regeneration in female brain. Menopause. 2018 Oct;25(10):1138-1151. |
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溶解性：
Soluble in DMSO |
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保存条件：
-20℃ |
配置溶液浓度参考：
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1mg |
5mg |
10mg |
| 1 mM |
2.699 ml |
13.496 ml |
26.992 ml |
| 5 mM |
0.54 ml |
2.699 ml |
5.398 ml |
| 10 mM |
0.27 ml |
1.35 ml |
2.699 ml |
| 50 mM |
0.054 ml |
0.27 ml |
0.54 ml |
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| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
北京