Norethindrone,68-22-4

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YZ剂描述：

产品名称：Norethindrone

产品别名：炔诺酮

英文别名：Norethisterone

靶点：Progesterone Receptor

CAS：68-22-4

纯度：>98%

外观：白色或类白色的结晶性粉末

保存方法：-20°C

描述：

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

溶解性：Ethanol ：5 mg/mL (16.75 mM)
DMSO ：56 mg/mL (187.7 mM)

体外研究：

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 () and two-fold stronger than progesterone. Binding and transactivation activities of NET for androgen receptor (5α-dihydrotestosterone ) are 3.2 and 1.1%, respectively, for estrogen receptor none (estradiol ) and for glucocorticoid receptor below 1% (dexamethasone ). 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.

体内研究：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.

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