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MifepristoneCayman Chemical Item Number 10006317
RU- 
Mifepristone (CAS 84371-65-3)
Description
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-
1 Cadepond, F., Ulmann, A., and Baulieu, E. RU486 (mifepristone): Mechanisms of action and clinical uses. Annu Rev Med 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. Proc Natl Acad Sci USA 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. J Steroid Biochem Mol Biol 53(1-6) 449-458 (1995).
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Gaddy, V.T., Barrett, J.T., Delk, J.N., et al. Mifepristone induces growth arrest, caspase activation, and apoptosis of estrogen receptor-
Background ReadingDelabre, K., Guiochon-Mantel, A., and Milgrom, E. In vivo evidence against the existence of antiprogestins disrupting receptor binding to DNA. Proc Natl Acad Sci USA 90 4421-4425 (1993). Edwards, D.P., Altmann, M., DeMarzo, A., et al. Progesterone receptor and the mechanism of action of progesterone antagonists. J Steroid Biochem Mol Biol 53(1-6) 449-458 (1995). 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). Cadepond, F., Ulmann, A., and Baulieu, E. RU486 (mifepristone): Mechanisms of action and clinical uses. Annu Rev Med 48 129-156 (1997). Gaddy, V.T., Barrett, J.T., Delk, J.N., et al. Mifepristone induces growth arrest, caspase activation, and apoptosis of estrogen receptor- Mifepristone is available in the following screening library: |
This product is available in custom sizes and/or larger quantities. Please contact our Sales Department for a quote or to purchase. Pricing updated 2012-05-25. Prices are subject to change without notice. To ask for assistance with one of our products please contact a Technical Support Scientist. Warning This product is not for human or veterinary use. Related ProductsShow all 14 Hide all but first 3Downloads
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