Norethisterone
产品说明书
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同义名 : | Norethindrone;NSC 9564;Norethindrone, Norethisterone, 19-nor-17α-ethynyltestosterone, Utovlan;SC 4640 |
| CAS号 : | 68-22-4 | |
| 货号 : | A542979 | |
| 分子式 : | C20H26O2 | |
| 纯度 : | 98% | |
| 分子量 : | 298.419 | |
| MDL号 : | MFCD00067596 | |
| 存储条件： |
Pure form Sealed in dry,2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 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 |
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| 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 |
| 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]. | ||
| 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 | - | - | |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.35mL 0.67mL 0.34mL |
16.75mL 3.35mL 1.68mL |
33.51mL 6.70mL 3.35mL |
| 参考文献 |
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