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Mifepristone

Basic information Description Safety Related Supplier

Mifepristone Basic information

Product Name:
Mifepristone
CAS:
84371-65-3
MF:
C29H35NO2
MW:
429.59
EINECS:
617-559-7
Mol File:
84371-65-3.mol
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Mifepristone Chemical Properties

Melting point:
195-198°C
alpha 
D20 +138.5° (c = 0.5 in chloroform)
Boiling point:
544.13°C (rough estimate)
Density 
1.0731 (rough estimate)
refractive index 
1.6290 (estimate)
storage temp. 
2-8°C
form 
Yellow solid
pka
12.94±0.60(Predicted)
Water Solubility 
474.8ug/L(22.5 ºC)
Merck 
14,6186
InChIKey
VKHAHZOOUSRJNA-GCNJZUOMSA-N
CAS DataBase Reference
84371-65-3(CAS DataBase Reference)
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Safety Information

Hazard Codes 
T
Risk Statements 
60-61
Safety Statements 
53-22-36/37/39-45
WGK Germany 
3
RTECS 
KG2955000
HS Code 
29372900
Hazardous Substances Data
84371-65-3(Hazardous Substances Data)
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Mifepristone Usage And Synthesis

Description

Mifepristone is a kind of antagonist of the progestational and glucocorticoid hormone. It is mainly used for the treatment of hypercortisolism in patients with nonpituitary cushing syndrome. During the treatment of Cushing’s syndrome, mifepristone takes effect through interfering with the binding of cortisol to its receptor. It reduces the effects of excess cortisol (e.g., high blood sugar levels) without causing decreased cortisol production. It can also be used to end a pregnancy. Its inhibition on progesterone can induce bleeding during the luteal phase and in early pregnancy.  

Description

Mifepristone is an orally-active progesterone and glucocorticoid receptor antagonist indicated for use as a post-coital contraceptive. In addition to being an abortifacient, mifepristone is reported to be effective in the treatment of ocular hypertension; its potential therapeutic effect in hormone-dependent tumors is currently under investigation.

Chemical Properties

Pale Yellow Solid

Originator

Roussel-Uclaf (France)

Uses

glutamate uptake inhibitor, AMPA blocker

Uses

A progesterone and glucocorticoid antagonist, suppresses VEGF production.

Uses

A progesterone receptor antagonist with partial agonist activity. Abortifacient.

Indications

Mifepristone is a progesterone receptor antagonist that has a high affinity for glucocorticoid receptors and little agonist effect.This drug has recently been approved for use in the United States for the treatment of hypercortisolism. At high doses, mifepristone blocks negative feedback of the hypothalamic–pituitary axis, thereby increasing endogenous corticotrophin and cortisol levels. Because mifepristone exerts its effects at the receptor level and not by altering glucocorticoid production, elevated serum cortisol and corticotrophin levels may not accurately reflect the effectiveness of the therapeutic regimen. Mifepristone does not inhibit cortisol binding to the mineralocorticoid receptor, so that the resulting corticotrophin disinhibition may cause potassium depletion. Thus, administration of a mineralocorticoid receptor antagonist such as spironolactone may be indicated with mifepristone. Hypoadrenalism, nausea, and drowsiness have been reported during prolonged administration of mifepristone.

brand name

Mifeprex (Danco);Ru-486;Mifegyne.

World Health Organization (WHO)

Mifepristone, an antiprogesterone used in combination with a prostaglandin for the termination of early pregnancy, was introduced in 1990. Use of the combination has been associated with episodes of coronary spasm that are attributed to administration of the prostaglandin and which have resulted in several cases of cardiac infarction and ventricular fibrillation. At least one of these incidents has been fatal.

Biological Activity

Selective antagonist at progesterone (PR) and glucocorticoid (GR) receptors in vitro and in vivo . Is a silent antagonist at PR and has a higher affinity than progesterone. Has higher affinity for GR than dexamethasone.

References

https://pubchem.ncbi.nlm.nih.gov/compound/mifepristone#section=Top
https://www.drugbank.ca/drugs/DB00834
https://www.drugs.com/cdi/mifepristone-tablets.html

Mifepristone Preparation Products And Raw materials

Raw materials

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MifepristoneSupplierMore

Nanjing Sunlida Biological Technology Co., Ltd. Gold
Tel:
025-58378339;025-57798810
Email:
sales@sunlidabio.com;sales@sunlidabio.com
Watson Biotechnology Co.,Ltd Gold
Tel:
027-59207879-
Email:
kf@3600chem.com
Zhengzhou Acme Chemical Co., Ltd. Gold
Tel:
0371-63312495-
Email:
3001379618@qq.com
Shanghai Boyle Chemical Co., Ltd.
Tel:
Email:
sales@boylechem.com
J & K SCIENTIFIC LTD.
Tel:
010-82848833- ;010-82848833-
Email:
jkinfo@jkchemical.com;market6@jkchemical.com
Basic information Description Safety Related Supplier