Nestoron

SKU: orb1302027

Description

Nestoron

Research Area

Metabolism Research

Key Properties

• CAS Number: 7759-35-5
• MW: 370.48
• Purity: 99.92%
• Formula: C₂₃H₃₀O₄
• SMILES: [H][C@@]12CC(=C)[C@](OC(C)=O)(C(C)=O)[C@@]1(C)CC[C@]1([H])[C@@]3([H])CCC(=O)C=C3CC[C@@]21[H]
• Target: Estrogen/progestogen Receptor,Progesterone Receptor
• Solubility: DMSO:55 mg/mL (148.46 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.4 mM)

Bioactivity

• Target IC50:
  PR:10.3 nM
• 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 .
• 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 . 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 .
• 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 .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Nestoron, Nestorone, Inhibitor, inhibit, NR3C3, Elcometrine, EstrogenReceptor, Estrogen Receptor, ProgesteroneReceptor, Progesterone Receptor, progestogen Receptor, progestogenReceptor, ST 1435, ST1435, ST-1435, Segesterone Acetate, PR

Compound Identifiers

PubChem CID

108059