| Name | Nestoron |
| Description | Nestoron (Segesterone Acetate), a synthetic progestin, is a high-affinity agonist of the progesterone receptor (EC50: 10.3 nM). |
| Animal Research | 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]. |
| In vitro | 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]. |
| In vivo | 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]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.4 mM), Sonication is recommended.
DMSO : 55 mg/mL (148.46 mM), Sonication is recommended.
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| Keywords | ST1435 | ST 1435 | progestogenReceptor | progestogen Receptor | ProgesteroneReceptor | Progesterone Receptor | PR | NR3C3 | Nestoron | Inhibitor | inhibit | EstrogenReceptor | Estrogen Receptor |
| Inhibitors Related | Tamoxifen | Mifepristone | Estradiol | Astragaloside IV | Estradiol benzoate | Bisphenol Z | 17α-Hydroxyprogesterone | Ethisterone | Alpha-Estradiol | Ferrous Bisglycinate | Megestrol acetate | Hinokitiol |
| Related Compound Libraries | Nuclear Receptor Compound Library | FDA-Approved & Pharmacopeia Drug Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Approved Drug Library | ReFRAME Related Library | Anti-Breast Cancer Compound Library | Drug Repurposing Compound Library | NO PAINS Compound Library | FDA-Approved Drug Library | Bioactive Compounds Library Max | Bioactive Lipid Compound Library |
United States
