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Norethindrone

Synonyms: Norethisterone

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

Norethindrone Chemical Structure

Norethindrone Chemical Structure

CAS: 68-22-4

Selleck's Norethindrone has been cited by 1 publication

Purity & Quality Control

Batch: S404001 DMSO] 60 mg/mL] false] Ethanol] 5 mg/mL] false] Water] Insoluble] false Purity: 99.79%
99.79

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Biological Activity

Description Norethindrone (Norethisterone) is a synthetic progestin, which mimic the actions of the endogenous ovarian hormone progesterone.
In vitro
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]
Cell Research 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.
In Vivo
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05293574 Not yet recruiting Ovarian Cyst Simple Assiut University October 1 2022 Phase 4
NCT05294341 Completed Contraception Milton S. Hershey Medical Center July 22 2022 Phase 4
NCT04016753 Completed Healthy Participants Bristol-Myers Squibb August 5 2019 Phase 1
NCT02905890 Completed Bacterial Vaginosis|HIV London School of Hygiene and Tropical Medicine|Imperial College London|University of Liverpool|MRC/UVRI and LSHTM Uganda Research Unit October 2 2017 Phase 4

Chemical lnformation & Solubility

Molecular Weight 298.42 Formula

C20H26O2
CAS No. 68-22-4 SDF Download Norethindrone SDF
Smiles CC12CCC3C(C1CCC2(C#C)O)CCC4=CC(=O)CCC34
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 60 mg/mL ( (201.05 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble


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In vivo
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