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Nestoron

Nestoron

产品编号 T5174   CAS 7759-35-5
别名: 醋酸烯诺孕酮, ST-1435, Segesterone Acetate, Nestorone, Elcometrine

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。

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Nestoron Chemical Structure
Nestoron, CAS 7759-35-5
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
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
MG-132限时半价
产品目录号及名称: Nestoron (T5174)
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 55 mg/mL (148.46 mM)

溶液配制表

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

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TargetMol Library Books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.
Pelargonidin-3-O-glucoside chloride Etonogestrel 17α-Hydroxyprogesterone Ospemifene Kaempferol WAY-200070 Estropipate Dehydrodiconiferyl alcohol

相关化合物库

该产品包含在如下化合物库中:
药物功能重定位化合物库 经典已知活性库 内分泌激素分子库 核受体化合物库 NO PAINS 化合物库 FDA上市及药典收录分子库 表型筛选靶点鉴定库 已知活性化合物库 上市药物库 人代谢物化合物库

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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。

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Keywords

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

 

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