Norethindrone

製品コードS4040 バッチS404001

印刷

化学情報

Chemical Structure Synonyms Norethisterone Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C20H26O2
分子量 298.42 CAS No. 68-22-4
Solubility (25°C)* 体外 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Human breast cancer cell MCF-7
濃度 0.1 nM - 1 mM
反応時間 7 days
実験の流れ 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.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。