| 货号 | 10006317-5000mg |
| 描述 | Progesterone is responsible for preparing the uterine lining for implantation of a fertilized ovum and to maintain pregnancy, eliciting its action through the nuclear progesterone receptor (PR). Mifepristone is a potent PR and glucocorticoid receptor (GR) antagonist with Ki values of approximately 1 nM.1 It is used in combination with misoprostol for the oral induction of first trimester abortions.1 Mifepristone promotes efficient binding of PR to hormone response elements (HRE) on DNA, but prevents transcriptional activation of the receptor.2,3,4 The IC50 of mifepristone for PR dimerization and activation is 0.6 nM; the IC50 for mifepristone-induced competitive binding of wild-type PR with a constitutively active PR for HRE is 0.01 nM.2 In anti-estrogen-resistant breast cancer cells, mifepristone induces growth arrest, caspase activation, and cell death, indicating the effectiveness of PR antagonism as a novel approach to treatment of select cancers.5 |
| 别名 | RU-486; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Cadepond, F.,Ulmann, A., and Baulieu, E.E. RU486 (mifepristone): Mechanisms of action and clinical uses. Annual Reviews of Medicine 48, 129-156 (1997). 2.Delabre, K.,Guiochon-Mantel, A., and Milgrom, E. In vivo evidence against the existence of antiprogestins disrupting receptor binding to DNA. Proceedings of the National Academy of Sciences of the United States of America 90, 4421-4425 (1993). 3.Beck, C.A.,Estes, P.A.,Bona, B.J., et al. The steroid antagonist RU486 exerts different effects on the glucocorticoid and progesterone receptors. Endocrinology 133(2), 728-740 (1993). 4.Edwards, D.P.,Altmann, M.,DeMarzo, A., et al. Progesterone receptor and the mechanism of action of progesterone antagonists. Journal of Steroid Biochemistry and Molecular Biology 53(1-6), 449-458 (1995). 5.Gaddy, V.T.,Barrett, J.T.,Delk, J.N., et al. Mifepristone induces growth arrest, caspase activation, and apoptosis of estrogen receptor-expressing, antiestrogen-resistant breast cancer cells. Clinical Cancer Research 10, 5215-5225 (2004). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 429.6 |
| 分子式 | C29H35NO2 |
| CAS号 | 84371-65-3 |
| 稳定性 | ≥ 2 years |
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