Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Nestoron (Segesterone Acetate) 是一种高度选择性和有效的孕激素,是一种 19-norprogesterone 衍生物,对progesterone receptors 具有高亲和力和选择性,可用作激素避孕药。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 297 | 现货 | ||
10 mg | ¥ 493 | 现货 | ||
25 mg | ¥ 987 | 现货 | ||
50 mg | ¥ 1,690 | 现货 | ||
100 mg | ¥ 2,550 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 463 | 现货 |
产品描述 | Nestoron (Segesterone Acetate), a synthetic progestin, is a high-affinity agonist of the progesterone receptor (EC50: 10.3 nM). |
靶点活性 | PR:10.3 nM |
体外活性 | Nestorone (ST-1435) showed significant binding (ED50 = 56 nM) compared to the binding of dexamethasone (ED50 = 21 nM) to calf thymus GR. Progesterone and Nestorone showed no binding to SHBG [1]. Chronic ST-1435 and E2 alone or in combination increased neurogenesis by a comparable magnitude, with minimum to no antagonistic or additive effects between ST-1435 and E2. In addition, chronic exposure of ST-1435 or ST-1435 + E2 stimulated oligodendrocyte generation [2]. |
体内活性 | 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 [1]. |
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 [1]. |
别名 | 醋酸烯诺孕酮, ST-1435, Segesterone Acetate, Nestorone, Elcometrine |
分子量 | 370.48 |
分子式 | C23H30O4 |
CAS No. | 7759-35-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 55 mg/mL (148.46 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6992 mL | 13.496 mL | 26.992 mL | 67.48 mL |
5 mM | 0.5398 mL | 2.6992 mL | 5.3984 mL | 13.496 mL | |
10 mM | 0.2699 mL | 1.3496 mL | 2.6992 mL | 6.748 mL | |
20 mM | 0.135 mL | 0.6748 mL | 1.3496 mL | 3.374 mL | |
50 mM | 0.054 mL | 0.2699 mL | 0.5398 mL | 1.3496 mL | |
100 mM | 0.027 mL | 0.135 mL | 0.2699 mL | 0.6748 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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20 g,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% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Nestoron 7759-35-5 Endocrinology/Hormones Others Estrogen/progestogen Receptor Progesterone Receptor Inhibitor 醋酸烯诺孕酮 ST-1435 Segesterone Acetate Nestorone ST 1435 inhibit NR3C3 ST1435 Elcometrine inhibitor