Norethindrone

Catalog No.S4040 Synonyms: Norethisterone

Norethindrone Chemical Structure

Molecular Weight(MW): 298.42

Norethindrone is a synthetic progestin, which mimic the actions of the endogenous ovarian hormone progesterone.

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In DMSO USD 130 In stock
USD 97 In stock
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Biological Activity

Description Norethindrone is a synthetic progestin, which mimic the actions of the endogenous ovarian hormone progesterone.
In vitro

Norethisterone, or, is a 19-nortestosterone derivative, that lacks a C19 methyl group and possesses C17 ethinyl substitution, and primarily displays progestational activity rather than androgenic activity and, to a lesser extent, has oestrogenic and anti-oestrogenic activity. [1] NET shows five- to eight-fold weaker progesterone receptor binding and transactivation activities than the Org 2058 (100%) and two-fold stronger than progesterone. Binding and transactivation activities of NET for androgen receptor (5α-dihydrotestosterone 100%) are 3.2 and 1.1%, respectively, for estrogen receptor none (estradiol 100%) and for glucocorticoid receptor below 1% (dexamethasone 100%). [2] Norethisterone (1 nM) inhibits serum-stimulated or oestradiol (0.1 nM)-induced proliferation of MCF-7 by 41% and 34%, respectively. [3] Norethisterone (50 nM) induces significant effects on rat osteoblast proliferation, differentiation, and mineralization processes, mimicking the effects of estradiol, which is mediated by estrogen receptor. [4]

In vivo Norethisterone displays hormonal properties in vivo. Mean active dose (MAD) of Norethisterone s.c. in progestagenic test (McPhail), androgenic test (Hershberger), estrogenic test (Allen–Doisy), and in a progestagenic and estrogenic test (ovulation inhibition test) is 0.63 mg/kg, 2.5 mg/kg, 4 mg/kg, and 0.235 mg/kg, respectively, and the MAD for orally administration is 0.25 mg/kg, 20 mg/kg, 8 mg/kg, and 12 mg/kg, respectively. [2] Norethisterone influences bone formation and resorption. Norethisterone (80 μg/day) decreased bone resorption in SO and OVX mice, while enhances estradiol-stimulated endosteal bone formation. [5] Norethisterone at the dose which is used in hormonal therapy for prevention of osteoporosis has a slight protective effect against bone mineral loss in castrated mice. [6]

Protocol

Cell Research:[3]
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  • Cell lines: Human breast cancer cell MCF-7
  • Concentrations: 0.1 nM - 1 mM
  • Incubation Time: 7 days
  • Method: 96 well plates are seeded with approximately 1000 MCF-7 cells per well in assay kit medium. Subsequently, the cells are incubated with medium containing charcoal/dextran treated serum for three days. The Norethisterone is then added alone to the wells and incubated for seven days. To mimic continuous combined HRT the cells are treated with an oestradiol (0.1 nM)/ Norethisterone combination for seven days. After incubation for seven days, cell proliferation is measured by using an ATP-chemosensitivity test. In brief, proliferation is quantified by measuring light emitted during the bioluminescence reaction of luciferine in the presence of ATP and luciferase.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 60 mg/mL (201.05 mM)
Ethanol 5 mg/mL (16.75 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 298.42
Formula

C20H26O2

CAS No. 68-22-4
Storage powder
Synonyms Norethisterone

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02905890 Not yet recruiting Bacterial Vaginosis|HIV London School of Hygiene and Tropical Medicine|Imperial College London|University of Liverpool|MRC/UVRI Uganda Research Unit on Aids January 2017 Phase 4
NCT02705963 Recruiting Solid Tumors Novartis Pharmaceuticals|Novartis October 2016 Phase 1
NCT02925494 Enrolling by invitation Uterine Fibroids|Heavy Menstrual Bleeding AbbVie September 2016 Phase 3
NCT02542410 Recruiting Endometriosis Boston Children’s Hospital May 2016 Phase 2
NCT02691494 Recruiting Uterine Fibroids|Heavy Menstrual Bleeding AbbVie February 2016 Phase 3
NCT02693002 Recruiting Menopause Gretchen Wells|University of Kentucky February 2016 Phase 4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID