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炔诺酮 /Norethisterone {[allProObj[0].p_purity_real_show]}

货号:A542979 同义名: Norethindrone;NSC 9564

Norethindrone is a synthetic progestin which can mimic the effects of endogenous ovarian hormones.

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Norethisterone 化学结构 CAS号:68-22-4
Norethisterone 化学结构
CAS号:68-22-4
Norethisterone 3D分子结构
CAS号:68-22-4
Norethisterone 化学结构 CAS号:68-22-4
Norethisterone 3D分子结构 CAS号:68-22-4
规格 价格 会员价 库存 数量
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Norethisterone 纯度/质量文件 产品仅供科研

货号:A542979 标准纯度: {[allProObj[0].p_purity_real_show]}
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Norethisterone 生物活性

描述 Progesterone Receptor (PGR) is a member or the steroid receptor superfamily. It mediates the physiological effects of progesterone, which plays a central role in reproductive events associated with the establishment and maintenance of pregnancy. Progesterone Receptor is involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Depending on the isoform, progesterone receptor functions as transcriptional activator or repressor. Norethindrone, also termed Norethisterone (NET) is a synthetic 19-nortestosterone derivative. Norethindrone acts as a ligand that binds to progesterone receptor. According to published data, mean of relative binding affinity (RBA) values of norethisterone to the progesterone, androgen and estrogen receptor in cytosol of human breast MCF-7 cells and to the glucocorticoid receptor in that of leukemic IM-9 cells were 21.5%, 3.2%, not binding, and 0.8%, respectively. These data were all expressed as percentage of standard ligands of Org 2058, 5a-dihydrotestosterone (DHT), estradiol (E2) and dexamethasone (Dex), respectively[3]. Mean of relative agonistic activity (RAA) values of norethisterone to the progesterone, androgen, estrogen and glucocorticoid receptor in transactivation assays with CHO cells using Org 2058, 5a-dihydro-testosterone (DHT), estradiol (E2) and dexamethasone (Dex) as standards were also measured. The data (also expressed as percentage of standard ligands) were 12.4%, and 1.1% respectively for the progesterone and androgen receptor, while no transactivation was detected for the estrogen or glucocorticoid receptor[3]. According to cell proliferation data measured by an ATP-chemosensitivity test, norethisterone inhibited MCF-7 cells proliferation between 23% and 41% over the concentration range of 0.01 nM to 10 μM tested. In vivo, the mean active doses (MAD) of norethisterone in progestagenic (McPhail), androgenic (Hershberger), estrogenic (Allen–Doisy) tests, and in a progestagenic and estrogenic (ovulation inhibition test) were 0.063 mg/kg, 2.5 mg/kg, 4 mg/kg and 0.235 mg/kg respectively after subcutaneous administration and 0.25 mg/kg, 20 mg/kg, 8 mg/kg and 12 mg/kg respectively after oral administration[3].

Norethisterone 动物研究

Dose Rat: 10 mg/kg, 50 mg/kg[3] (p.o.), 8 mg/kg[2] (p.o.); 4 mg/kg[2] (s.c.)
Administration p.o., s.c.

Norethisterone 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01129102 Dysmenorrhea Phase 3 Completed - -
NCT01466114 Relapsing-remitting Multiple S... 展开 >>clerosis Secondary-progressive Multiple Sclerosis Primary-progressive Multiple Sclerosis 收起 << Phase 2 Recruiting December 2018 United States, California ... 展开 >> University of California Los Angeles Recruiting Los Angeles, California, United States, 90095 Contact: Mike Montag, M.S.    310-206-2176    MMontag@mednet.ucla.edu    Sub-Investigator: Barbara Giesser, MD          Sub-Investigator: Callene Momtazee, MD          United States, Colorado The University of Colorado Denver Completed Aurora, Colorado, United States, 80045 United States, New Mexico The University of New Mexico Completed Albuquerque, New Mexico, United States, 87131 United States, Pennsylvania The University of Pennsylvania Recruiting Philadelphia, Pennsylvania, United States, 19104 Contact: Amber Roberts    215-662-4893    daj37@mail.med.upenn.edu    Principal Investigator: Dina Jacobs, M.D. 收起 <<
NCT01129102 - Completed - -

Norethisterone 参考文献

[1]Schindler AE, Campagnoli C, et al. Classification and pharmacology of progestins. Maturitas. 2003 Dec 10;46 Suppl 1:S7-S16.

[2]Schoonen WG, Deckers GH, et al. Hormonal properties of norethisterone, 7alpha-methyl-norethisterone and their derivatives. J Steroid Biochem Mol Biol. 2000 Nov 15;74(4):213-22.

[3]Schoonen WG, Deckers GH, de Gooijer ME, de Ries R, Kloosterboer HJ. Hormonal properties of norethisterone, 7alpha-methyl-norethisterone and their derivatives. J Steroid Biochem Mol Biol. 2000 Nov 15;74(4):213-22. doi: 10.1016/s0960-0760(00)00125-4. PMID: 11162927.

Norethisterone 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.35mL

0.67mL

0.34mL

16.75mL

3.35mL

1.68mL

33.51mL

6.70mL

3.35mL

Norethisterone 技术信息

CAS号68-22-4
分子式C20H26O2
分子量 298.419
别名 Norethindrone;NSC 9564;Norethindrone, Norethisterone, 19-nor-17α-ethynyltestosterone, Utovlan;SC 4640
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 25 mg/mL(83.77 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 2.5 mg/mL(8.38 mM),配合低频超声助溶

动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 2 mg/mL clear

PO 0.5% CMC-Na 30 mg/mL suspension

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