Mifepristone Inhibitor CAS No. 84371-65-3

Cat. No.	Name	Size	Price	Add Cart
KI0671	Mifepristone	50 mg	$230

Chemical Characteristic

Product Name	Mifepristone
CAS No.	84371-65-3
Molecular Weight	429.6
Formula	C₂₉H₃₅NO₂
Chemical Structure

Biological activities

Mifepristone is a selective antagonist at progesterone (PR) and glucocorticoid (GR) receptors with IC50 values of 307 and 100 nM, respectively. The Kd values of mifepristone are 40 and 15 nM against PR and GR, respectively. In osteosarcoma cells, mifepristone reveals a higher potency than cyproterone acetate to prevent responses to dexamethasone-induced GR transactivation and NF-κB transrepression.^[1] Mifepristone inhibits human blastocyst attachment to an in vitro endometrial three-dimensional cell culture model.^[2] In vitro, mifepristone also down-regulates the expressions of estrogen receptor and progesterone receptor in both the eutopic and the ectopic endometrial cells.^[3] Mifepristone effectively induces apoptosis in human LNCaP prostate cancer cells in culture.^[4] In the mouse models bearing xenografted cisplatin-resistant ovarian carcinoma in vivo, combined treatment with mifepristone and cisplatin results in significantly greater inhibition rates of the tumors compared to exclusive cisplatin treatment.^[5] In a created GAL4/ΔN-IκBα transgenic mice, mifepristone treatment (5 mg/kg) induces expression of a deletion mutant of IκBα in hepatocytes.^[6]

Protocols

In vivo: Mifepristone is dissolved in sesame oil.^[6]

References

[1] Honer C, et al. Glucocorticoid receptor antagonism by cyproterone acetate and RU486. Mol Pharmacol. 2003, 63(5): 1012-1020. [2] Lalitkumar PG, et al. Mifepristone, but not levonorgestrel, inhibits human blastocyst attachment to an in vitro endometrial three-dimensional cell culture model. Hum Reprod. 2007, 22(11): 3031-3037. [3] Jiang J, et al. Effect of mifepristone on estrogen and progesterone receptors in human endometrial and endometriotic cells in vitro. Fertil Steril. 2002, 77(5): 995-1000. 閵嗏偓閵嗏偓 [4] El Etreby MF, et al. Induction of apoptosis by mifepristone and tamoxifen in human LNCaP prostate cancer cells in culture. Prostate. 2000, 43(1): 31-42. 閵嗏偓閵嗏偓 [5] Liu Y, et al. Enhancement of antitumor effect of cisplatin against human ovarian carcinoma cells by mifepristone in vivo. Di Yi Jun Yi Da Xue Xue Bao. 2003, 23(3): 242-244. 閵嗏偓閵嗏偓 [6] Chaisson ML, et al. Hepatocyte-specific inhibition of NF-kappaB leads to apoptosis after TNF treatment, but not after partial hepatectomy. J Clin Invest. 2002, 110(2): 193-202. 閵嗏偓閵嗏偓

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