Norethindrone

Catalog No.S4040 Batch:S404001

Technical Data

Formula	C₂₀H₂₆O₂
Molecular Weight	298.42	CAS No.	68-22-4
Solubility (25°C)*	In vitro	DMSO	60 mg/mL (201.05 mM)
		Ethanol	5 mg/mL (16.75 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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	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 (from reference)

Cell Assay:^{^[3]}	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.

Cell Assay:^{^[3]}

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.

References

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Selleck's Norethindrone has been cited by 1 publication

Discovering the anti-cancer potential of non-oncology drugs by systematic viability profiling [ Nat Cancer, 2020, 1(2):235-248]	PubMed: 32613204

Discovering the anti-cancer potential of non-oncology drugs by systematic viability profiling [ Nat Cancer, 2020, 1(2):235-248]

PubMed: 32613204

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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