84371-65-3 Mifeprex Progesterone Steroid Hormone Mifepristone for Abortion


Quick Detail:

Product Name	Mifepristone
CAS NO	84371-65-3
MF	C29H35NO2
MW	429.59
Mol File	84371-65-3. Mol
storage temp	2-8°C
Usage	A progesterone receptor antagonist with partial agonist activity. Abortifacient.
Chemical Properties	Pale Yellow Solid
mp	195-198°C
Merck	6186
Package	1kg/aluminium foil bag or as required
Shipping	EMS , DHL , TNT , FedEx , UPS
Delivery time	within 24 hours upon receipt of payment.
Synonyms	11-(4-(dimethylamino)phenyl)-17-hydroxy-17-(1-propynyl)-estra-9-dien-3-one; 11beta-[4-(n, n-dimethylamino)phenyl]-17alpha-(prop-1-ynyl)-delta4,9-estradiene; 17-beta)-(11-bet; 17beta)-11-[4-(dimethylamino)-phenyl]-17-hydroxy-17-(1-propynyl)estra-(11bet; 17-beta-hydroxy-11-beta-(4-dimethylaminophenyl-1)-17-alpha-(prop-1-ynyl)oest; -17beta-ol-3-one; 4,9-dien-3-one; r38486

Product Description:

1. Mifepristone, sold commercially under the name Mifeprex, also is known as RU-486, the abortion pill, the early option pillfor medical abortion. While it has been used for many years in Europe, mifepristone has only been available for use in theUnited States since the U. S. Food and Drug Administration (FDA) approved it in 2000 for use in abortion. More than37,000 abortions were performed using the pill in the first six months of 2001.

2. This drug causes pregnancy to end by blocking the female hormone progesterone. The lack of progesterone makes theuterus shed its lining, which causes bleeding similar to a menstrual period. Three days after taking mifepristone, womenare given a second drug, misprostol, to cause uterine contractions that expel the contents of the uterus. Most women areable remain in their own home while they pass the fetus.

Application:

1. Mifepristone belongs to the anti-progesterone drug. It was first successfully developed by the French company Roussel-Uolsf in the early 1980s for acting as a novel anti-fertility drug acting at receptor levels. It has no progesterone, testosterone, estrogen activity. It first entered into market in France at 1988 with its major role in acting on the endometrial progesterone receptor which is capable of binding with the progesterone receptor and glucocorticoid receptor with high affinity. The affinity to the endometrial progesterone receptor of it is five time as strong as that of progesterone without significant effects on the cortisol levels, and can produce a strong anti-progesterone effect thus causing the degeneration of decidua and chorionic villi of pregnancy.

2. It can also cause release of endogenous prostaglandins which causes uterine contractions while resulting in the decreased production of the human chorionic gonadotropin hormones and dissolution of corpus luteum, and finally causing the embryo abortion. Because the drug can't trigger enough uterine activity so single application for anti-pregnancy yields a relative high rate of incomplete abortion, but it can increase uterine sensitivity to prostaglandins, so that it not only reduces the adverse effects of prostaglandins after adding a small dose of prostaglandin but also make the complete abortion rate increased significantly. In addition mifepristone also has a softening and expansion effect of the cervix.

3. Mifepristone is rapidly absorbed after oral administration with a bioavailability being 70% and a plasma protein binding rate of 98%. The plasma concentration reaches peak at 0.7 to 1 hours after oral administration with duration of 12 hours and being non-detective after 48 hours. It has a half-life of 24 to 33 hours. It is mainly distributed in the brain and pituitary gland, adrenal cortex and endometrium. More than 90% of this product is metabolized by the liver into the bile and further excreted by the digestive tract, 10% is excreted by the urinary tract. It can be clinically used for anti-pregnancy, inducing menstruation, post-coital contraception, abortion and stillbirth cervical ripening, but also for gynecological surgical procedures, such as IUD placement and removal, taking samples of endometrial, laser separation of cervical dysplasia, and cervical dilation as well as curettage.


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