An antagonist of glucocorticoid

Mifepristone – 1 g

Brand:
Cayman
CAS:
84371-65-3
Storage:
-20
UN-No:
Non-Hazardous - /

Mifepristone is an antagonist of glucocorticoid, progesterone, and androgen receptors (Kis = 0.1, 0.64, and 0.65 nM, respectively).{41967,41968,40657} It is selective for these receptors over the mineralocorticoid receptor (MR), estrogen receptor α (ERα), and ERβ (Kis = 640, >200, and >750 nM, respectively).{41967} In cell-based assays, mifepristone inhibits alkaline phosphatase activity stimulated by the progesterone receptor agonist R5020 as well as reporter transcription stimulated by either dexamethasone (Item No. 11015) or R5020 (IC50s = 7, 5.9, and 1.3 nM, respectively).{40657} It also inhibits synthetic androgen R1881-stimulated reporter transcription in a concentration-dependent manner.{41968} Mifepristone (10 µM) inhibits growth of 4-OHT-resistant MCF-7 breast cancer cells in vitro.{12451} It also inhibits tumor growth in an SKOV3 ovarian cancer nude mouse xenograft model when administered at doses of 0.5 or 1 mg per day.{41969} Formulations containing mifepristone have been used for the induction of medical abortions.  

 

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SKU: 10006317 - 1 g Category:

Description

An antagonist of glucocorticoid, progesterone, and androgen receptors (Kis = 0.1, 0.64, and 0.65 nM, respectively); selective for these receptors over MR, ERα, and ERβ (Kis = 640, >200, and >750 nM, respectively); inhibits R5020-stimulated alkaline phosphatase activity as well as reporter transcription stimulated by either dexamethasone or R5020 in cell-based assays (IC50s = 7, 5.9, and 1.3 nM, respectively); inhibits R1881-stimulated reporter transcription in a concentration-dependent manner; inhibits growth of 4-OHT-resistant MCF-7 breast cancer cells in vitro at 10 µM; inhibits tumor growth in an SKOV3 ovarian cancer nude mouse xenograft model at 0.5 or 1 mg per day

Formal name: 11β-[4-(dimethylamino)phenyl]-17β-hydroxy-17-(1-propynyl)-estra-4,9-dien-3-one

Synonyms:  RU-486

Molecular weight: 429.6

CAS: 84371-65-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Lipids|Sterol Lipids||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cancer|Multidrug Resistance||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Androgens||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Estrogens & Progestins||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Glucocorticoids & Mineralocorticoids||Research Area|Endocrinology & Metabolism|Reproductive Biology

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