Catalog No.S4040 Synonyms: Norethisterone
Molecular Weight(MW): 298.42
Norethindrone is a synthetic progestin, which mimic the actions of the endogenous ovarian hormone progesterone.
Purity & Quality Control
|Description||Norethindrone is a synthetic progestin, which mimic the actions of the endogenous ovarian hormone progesterone.|
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.  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%).  Norethisterone (1 nM) inhibits serum-stimulated or oestradiol (0.1 nM)-induced proliferation of MCF-7 by 41% and 34%, respectively.  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. 
|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.  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.  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. |
-  Schindler AE, et al. Maturitas, 2003, 46 Suppl 1, S7-S16.
-  Schoonen WG, et al. J Steroid Biochem Mol Biol, 2000, 74(4), 213-222.
-  Seeger H, et al. J Br Menopause Soc, 2003, 9(1), 36-38.
|In vitro||DMSO||60 mg/mL (201.05 mM)|
|Ethanol||5 mg/mL (16.75 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01817530||Completed||Heavy Uterine Bleeding|Uterine Fibroids||AbbVie||April 8 2013||Phase 2|
|NCT03213457||Recruiting||Endometriosis||AbbVie||July 7 2017||Phase 3|
|NCT02691494||Active not recruiting||Uterine Fibroids|Heavy Menstrual Bleeding||AbbVie||January 4 2016||Phase 3|
|NCT03353857||Active not recruiting||Biological Availability||Bayer||November 29 2017||Phase 1|
|NCT00184795||Completed||Menopause|Menopausal Vasomotor Symptoms||Novo Nordisk A/S||May 28 2004||Phase 3|
|NCT03343067||Recruiting||Endometriosis||AbbVie||December 27 2017||Phase 3|
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