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Nestoron

Catalog No. T5174 CAS 7759-35-5

Synonyms: ST-1435, Segesterone Acetate, Nestorone, Elcometrine

Nestoron (Segesterone Acetate), a synthetic progestin, is a high-affinity agonist of the progesterone receptor (EC50: 10.3 nM).

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Nestoron, CAS 7759-35-5

Pack Size	Availability	Price/USD
5 mg	In stock	$ 35.00
10 mg	In stock	$ 57.00
25 mg	In stock	$ 118.00
50 mg	In stock	$ 226.00
100 mg	In stock	$ 365.00
1 mL * 10 mM (in DMSO)	In stock	$ 63.00

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Purity: 99.83%

Purity: 99.48%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Nestoron (Segesterone Acetate), a synthetic progestin, is a high-affinity agonist of the progesterone receptor (EC50: 10.3 nM).
Targets&IC50	PR:10.3 nM
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].
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].

Synonyms	ST-1435, Segesterone Acetate, Nestorone, Elcometrine
Molecular Weight	370.48
Formula	C23H30O4
CAS No.	7759-35-5

Storage

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

Solubility Information

DMSO: 55 mg/mL (148.46 mM)

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library FDA-Approved Drug Library Endocrinology-Hormone Compound Library FDA-Approved & Pharmacopeia Drug Library Bioactive Compound Library Bioactive Compounds Library Max Human Metabolite Library NO PAINS Compound Library Nuclear Receptor Compound Library Target-Focused Phenotypic Screening Library

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Keywords

Nestoron 7759-35-5 Endocrinology/Hormones Others Estrogen/progestogen Receptor Progesterone Receptor Inhibitor ST-1435 Segesterone Acetate Nestorone ST 1435 inhibit NR3C3 ST1435 Elcometrine inhibitor

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