Synonyms: Estra-4, 9-dien-3-one, 11-[4-(dimethylamino)- phenyl]-17-hydroxy-17-(1-propynyl)-, (11a, – 17a)-Mifepristone; 17-beta-Hydroxy-11-beta-(4-dimethylaminophenyl-1)-17-alpha-(prop-1-ynyl)oestra-4, 9-dien-3-one
Inchi: InChI=1S/C29H35NO2/c1-5-15-29(32)16-14-26-24-12-8-20-17-22(31)11-13-23(20)27(24)25(18-28(26, 29)2)19-6-9-21(10-7-19)30(3)4/h6-7, 9-10, 17, 24-26, 32H, 8, 11-14, 16, 18H2, 1-4H3/t24-, 25+, 26-, 28-, 29-/m0/s1
CAS No.: 84371-65-3
Density: 1.18 g/cm3
Melting Point: 195-198° C
Boiling Point: 628.6 ° C at 760 mmHg
Refractive Index: 1.623
Flash Point: 334 ° C
Appearance: Pale Yellow Solid
Grade: Pharmaceutical Grade
Storage: Shading, confined preservation
Lead time: Within 12 hours upon receipt of payment
Delivery: EMS, DHL, TNT, FedEx, UPS
Usage: New anti-progesterone, and has anti-glucocorticoid activity, but not progesterone, estrogen, androgen and anti-estrogen activity. And progesterone receptor affinity 5-fold stronger than progesterone. For anti-early pregnancy, reminders by only pregnancy, fetal death, uterine induction of labor, etc.
Mifepristone (or RU-486) is a synthetic steroid compound with both antiprogesterone and antiglucocorticoid properties. The compound is a 19-nor steroid with substitutions at positions C11 and C17 (17 beta-hydroxy-11 beta-[4-dimethylamino phenyl] 17 alpha-[1-propynyl]estra-4, 9-dien-3-one), which antagonizes cortisol action competitively at the receptor level.
Mifepristone is a progesterone receptor antagonist used as an abortifacient in the first months of pregnancy, and in smaller doses as an emergency contraceptive. It is also a powerful glucocorticoid receptor antagonist, and has occasionally been used in refractory Cushing’s syndrome (due to ectopic/neoplastic ACTH/cortisol secretion).
Mifepristone was the first antiprogestin to be developed and it has been evaluated extensively for its use as an abortifacient.
Mifepristone can also be used in smaller doses as an emergency contraceptive; If taken after sex but before ovulation, it can prevent ovulation and so prevent pregnancy. In this role, a 10-mg dose is not as effective as the 600-mg dose, but has fewer side effects. Mifeprex and Mifegyne are only available in 200-mg tablets.
A review of studies in humans found that the contraceptive effects of the 10-mg dose were probably due mainly to its effects on ovulation, and not inhibition of implantation, but “the knowledge of the mechanism of action remains incomplete”. Treatment with 200 mg of mifepristone changes steroid receptor expression in the Fallopian tube, inhibits endometrial development, and effectively prevents implantation.
Other medical applications of mifepristone studied in clinical trials include regular long-term use as an oral contraceptive, and treatment of HIV infection, uterine fibroids, endometriosis, major depression with psychotic features, bipolar depression and disorders causing cognitive dysfunction, post-traumatic stress disorder, chronic multisymptom illness, glaucoma, meningiomas, breast cancer, ovarian cancer, and prostate cancer.