Réactifs et instruments pour l'immunologie, la biologie cellulaire et la biologie moléculaire.

Mifepristone [84371-65-3]

Imprimer

Référence HY-13683-100mg

Conditionnement : 100mg

Marque : MedChemExpress

Demander plus d'informations

Description

Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC₅₀s of 0.2 nM and 2.6 nM in in vitro assay^[1].

IC₅₀ & Target

Human Endogenous Metabolite

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	1.6 nM Compound: Mifepristone	Antagonist activity at human glucocorticoid receptor assessed as inhibition of corticoid-induced transcription in human A549 cells by GRE-linked luciferase reporter gene assay Antagonist activity at human glucocorticoid receptor assessed as inhibition of corticoid-induced transcription in human A549 cells by GRE-linked luciferase reporter gene assay	[PMID: 17317167]
A549	IC₅₀	1.6 nM Compound: Mifepristone	Antagonist activity at glucocorticoid receptor in human A549 cells assessed as inhibition of corticoid-induced transcription after 16 hrs by glucocorticoid response element-driven luciferase reporter gene assay Antagonist activity at glucocorticoid receptor in human A549 cells assessed as inhibition of corticoid-induced transcription after 16 hrs by glucocorticoid response element-driven luciferase reporter gene assay	[PMID: 19217285]
A549	IC₅₀	1.6 nM Compound: Mifepristone	Antagonist activity at glucocorticoid receptor in human A549 cells assessed as inhibition of corticoid-induced GRE-linked luciferase reporter gene activity Antagonist activity at glucocorticoid receptor in human A549 cells assessed as inhibition of corticoid-induced GRE-linked luciferase reporter gene activity	[PMID: 17169557]
A549	IC₅₀	6 nM Compound: 1, mifepristone,RU-486	Antagonist activity at glucocorticoid receptor expressed in A549 cells assessed as inhibition of corticoid-induced gene transcription by luciferase reporter gene assay Antagonist activity at glucocorticoid receptor expressed in A549 cells assessed as inhibition of corticoid-induced gene transcription by luciferase reporter gene assay	[PMID: 17855092]
CHO	IC₅₀	5 nM Compound: 1, RU-486	Activity at GR expressed in CHO cells assessed as decrease in dexamethasone-stimulated alkaline phosphatase production by GRAF assay Activity at GR expressed in CHO cells assessed as decrease in dexamethasone-stimulated alkaline phosphatase production by GRAF assay	[PMID: 16987661]
CHO	IC₅₀	5 nM Compound: 1 Mifepristone - RU-486	Inhibition of Dexamethasone stimulated transcriptional activity in CHO cells expressing glucocorticoid receptor Inhibition of Dexamethasone stimulated transcriptional activity in CHO cells expressing glucocorticoid receptor	[PMID: 12824023]
CHO-K1	IC₅₀	0.008 nM Compound: 4 (Mifepristone)	Inhibition of CHO-K1 cells expressing glucocorticoid receptor Inhibition of CHO-K1 cells expressing glucocorticoid receptor	[PMID: 15456242]
CHO-K1	IC₅₀	0.4 nM Compound: 1	Antagonist activity at human progesterone receptor expressed in CHO-K1 cells harboring firefly luciferase gene after 20 hrs by One-Glo luciferase reporter gene assay Antagonist activity at human progesterone receptor expressed in CHO-K1 cells harboring firefly luciferase gene after 20 hrs by One-Glo luciferase reporter gene assay	[PMID: 31274313]
CHO-K1	IC₅₀	3.26 nM Compound: 1	Antagonist activity at human glucocorticoid receptor expressed in CHO-K1 cells harboring firefly luciferase gene after 20 hrs by One-Glo luciferase reporter gene assay Antagonist activity at human glucocorticoid receptor expressed in CHO-K1 cells harboring firefly luciferase gene after 20 hrs by One-Glo luciferase reporter gene assay	[PMID: 31274313]
CHO-K1	IC₅₀	3.5 nM Compound: 1	Antagonist activity at human glucocorticoid receptor expressed in CHO-K1 cells assessed as inhibition of glucocorticoid receptor-dexamethasone coactivator protein-protein interaction incubated for 24 hrs by bioluminescence assay Antagonist activity at human glucocorticoid receptor expressed in CHO-K1 cells assessed as inhibition of glucocorticoid receptor-dexamethasone coactivator protein-protein interaction incubated for 24 hrs by bioluminescence assay	[PMID: 31274313]
CHO-K1	IC₅₀	7.8 nM Compound: 4 (Mifepristone)	Inhibition of AR-dimerization in CHO-K1 cells expressing human androgen receptor Inhibition of AR-dimerization in CHO-K1 cells expressing human androgen receptor	[PMID: 15456242]
COS-7	IC₅₀	0.6 nM Compound: 1, mifepristone	Antagonist activity at cloned glucocorticoid receptor-ligand binding domain expressed in african green monkey COS7 cells by GAL4 luciferase reporter assay Antagonist activity at cloned glucocorticoid receptor-ligand binding domain expressed in african green monkey COS7 cells by GAL4 luciferase reporter assay	[PMID: 18504132]
COS-7	IC₅₀	0.6 nM Compound: 3, mifepristone	Antagonist activity at human GR ligand binding domain expressed in african green monkey COS7 cells in presence of Dexamethasone by Gal4 hybrid assay Antagonist activity at human GR ligand binding domain expressed in african green monkey COS7 cells in presence of Dexamethasone by Gal4 hybrid assay	[PMID: 18318463]
COS-7	IC₅₀	3.2 nM Compound: Mifepristone	Antagonist activity at glucocorticoid receptor ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay Antagonist activity at glucocorticoid receptor ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay	[PMID: 19863083]
COS-7	IC₅₀	5 μM Compound: 1, mifepristone	Antagonist activity at cloned estrogen receptor-ligand binding domain expressed in african green monkey COS7 cells by GAL4 luciferase reporter assay Antagonist activity at cloned estrogen receptor-ligand binding domain expressed in african green monkey COS7 cells by GAL4 luciferase reporter assay	[PMID: 18504132]
COS-7	IC₅₀	5000 nM Compound: 1, mifepristone	Antagonist activity at cloned estrogen receptor-ligand binding domain expressed in african green monkey COS7 cells by GAL4 luciferase reporter assay Antagonist activity at cloned estrogen receptor-ligand binding domain expressed in african green monkey COS7 cells by GAL4 luciferase reporter assay	[PMID: 18504132]
COS-7	IC₅₀	590 nM Compound: 1, mifepristone	Antagonist activity at cloned mineralocorticoid receptor-ligand binding domain expressed in african green monkey COS7 cells by GAL4 luciferase reporter assay Antagonist activity at cloned mineralocorticoid receptor-ligand binding domain expressed in african green monkey COS7 cells by GAL4 luciferase reporter assay	[PMID: 18504132]
COS-7	IC₅₀	6.9 nM Compound: 1, mifepristone	Antagonist activity at cloned androgen receptor-ligand binding domain expressed in african green monkey COS7 cells by two hybrid luciferase assay Antagonist activity at cloned androgen receptor-ligand binding domain expressed in african green monkey COS7 cells by two hybrid luciferase assay	[PMID: 18504132]
COS-7	IC₅₀	6.9 nM Compound: 3, mifepristone	Antagonist activity at human AR ligand binding domain expressed in african green monkey COS7 cells in presence of 5-alpha-dihydrotestosterone by Gal4 hybrid assay Antagonist activity at human AR ligand binding domain expressed in african green monkey COS7 cells in presence of 5-alpha-dihydrotestosterone by Gal4 hybrid assay	[PMID: 18318463]
CV-1	EC₅₀	>10000 nM Compound: RU-486	Agonist activity at human ERalpha expressed in african green monkey CV1 cells co-transfected with ERE-MMTV-Luc after 24 hrs by luciferase reporter gene assay Agonist activity at human ERalpha expressed in african green monkey CV1 cells co-transfected with ERE-MMTV-Luc after 24 hrs by luciferase reporter gene assay	[PMID: 20510622]
CV-1	EC₅₀	>10000 nM Compound: RU-486	Agonist activity at human ERbeta expressed in african green monkey CV1 cells co-transfected with ERE-MMTV-Luc after 24 hrs by luciferase reporter gene assay Agonist activity at human ERbeta expressed in african green monkey CV1 cells co-transfected with ERE-MMTV-Luc after 24 hrs by luciferase reporter gene assay	[PMID: 20510622]
CV-1	EC₅₀	>10000 nM Compound: RU-486	Agonist activity at human mineralocorticoid receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc after 24 hrs by luciferase reporter gene assay Agonist activity at human mineralocorticoid receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc after 24 hrs by luciferase reporter gene assay	[PMID: 20510622]
CV-1	EC₅₀	>10000 nM Compound: RU-486	Agonist activity at human progesterone receptor B expressed in african green monkey CV1 cells co-transfected with MMTV-Luc after 24 hrs by luciferase reporter gene assay Agonist activity at human progesterone receptor B expressed in african green monkey CV1 cells co-transfected with MMTV-Luc after 24 hrs by luciferase reporter gene assay	[PMID: 20510622]
CV-1	EC₅₀	>10 μM Compound: RU-486	Agonist activity at human ERalpha expressed in african green monkey CV1 cells co-transfected with ERE-MMTV-Luc after 24 hrs by luciferase reporter gene assay Agonist activity at human ERalpha expressed in african green monkey CV1 cells co-transfected with ERE-MMTV-Luc after 24 hrs by luciferase reporter gene assay	[PMID: 20510622]
CV-1	EC₅₀	0.3 nM Compound: Mifepristone	Antagonistic activity at human progesterone receptor in CV-1 cells. Antagonistic activity at human progesterone receptor in CV-1 cells.	[PMID: 12781198]
CV-1	EC₅₀	0.6 nM Compound: mifepristone	Antagonist activity at human GR expressed in CV1 cells by GRE activation assay Antagonist activity at human GR expressed in CV1 cells by GRE activation assay	[PMID: 17705362]
CV-1	EC₅₀	10 nM Compound: RU-486	Agonist activity at human androgen receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc after 24 hrs by luciferase reporter gene assay Agonist activity at human androgen receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc after 24 hrs by luciferase reporter gene assay	[PMID: 20510622]
CV-1	EC₅₀	872 nM Compound: RU-486	Agonist activity at human glucocorticoid receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc after 24 hrs by luciferase reporter gene assay Agonist activity at human glucocorticoid receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc after 24 hrs by luciferase reporter gene assay	[PMID: 20510622]
CV-1	IC₅₀	>1000 nM Compound: RU-486	Antagonist activity at human ERalpha expressed in african green monkey CV1 cells co-transfected with ERE-MMTV-Luc by luciferase reporter gene assay Antagonist activity at human ERalpha expressed in african green monkey CV1 cells co-transfected with ERE-MMTV-Luc by luciferase reporter gene assay	[PMID: 20510622]
CV-1	IC₅₀	>10000 nM Compound: RU-486	Antagonist activity at human mineralocorticoid receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc by luciferase reporter gene assay Antagonist activity at human mineralocorticoid receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc by luciferase reporter gene assay	[PMID: 20510622]
CV-1	IC₅₀	>1 μM Compound: RU-486	Antagonist activity at human ERalpha expressed in african green monkey CV1 cells co-transfected with ERE-MMTV-Luc by luciferase reporter gene assay Antagonist activity at human ERalpha expressed in african green monkey CV1 cells co-transfected with ERE-MMTV-Luc by luciferase reporter gene assay	[PMID: 20510622]
CV-1	IC₅₀	>10 μM Compound: RU-486	Antagonist activity at human mineralocorticoid receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc by luciferase reporter gene assay Antagonist activity at human mineralocorticoid receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc by luciferase reporter gene assay	[PMID: 20510622]
CV-1	IC₅₀	0.18 nM Compound: RU-486 (Mifepristone)	Antagonistic activity against human progesterone receptor B (hPR-B) in co-transfected CV-1 cells. Antagonistic activity against human progesterone receptor B (hPR-B) in co-transfected CV-1 cells.	[PMID: 9484511]
CV-1	IC₅₀	0.18 nM Compound: RU-486 Mifepristone	Concentration required to give half-maximal inhibition against human Progesterone receptor B isoform in co-transfected CV-1 cell lines. Concentration required to give half-maximal inhibition against human Progesterone receptor B isoform in co-transfected CV-1 cell lines.	[PMID: 8627601]
CV-1	IC₅₀	0.3 nM Compound: 1	Antagonist activity against progesterone receptor (PR) using PRE-luciferase plasmid co-transfected CV-1 cells Antagonist activity against progesterone receptor (PR) using PRE-luciferase plasmid co-transfected CV-1 cells	[PMID: 12238914]
CV-1	IC₅₀	0.3 nM Compound: Mifepristone	Inhibitory concentration for antagonistic activity towards human progesterone receptor (hPR) using the cotransfection assay in CV-1 cells Inhibitory concentration for antagonistic activity towards human progesterone receptor (hPR) using the cotransfection assay in CV-1 cells	[PMID: 12781197]
CV-1	IC₅₀	0.3 nM Compound: 1	Antagonist activity against human progesterone receptor B (hPR-B) in co-transfected CV-1 cells Antagonist activity against human progesterone receptor B (hPR-B) in co-transfected CV-1 cells	[PMID: 9873612]
CV-1	IC₅₀	0.6 nM Compound: RU-486	Antagonist activity at human progesterone receptor B expressed in african green monkey CV1 cells co-transfected with MMTV-Luc assessed as effect on progesterone-induced activity by luciferase reporter gene assay Antagonist activity at human progesterone receptor B expressed in african green monkey CV1 cells co-transfected with MMTV-Luc assessed as effect on progesterone-induced activity by luciferase reporter gene assay	[PMID: 20510622]
CV-1	IC₅₀	0.95 nM Compound: RU-486	Antagonist activity at human glucocorticoid receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc by luciferase reporter gene assay Antagonist activity at human glucocorticoid receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc by luciferase reporter gene assay	[PMID: 20510622]
CV-1	IC₅₀	1 nM Compound: RU-486	Antagonist activity at human androgen receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc by luciferase reporter gene assay Antagonist activity at human androgen receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc by luciferase reporter gene assay	[PMID: 20510622]
CV-1	IC₅₀	10 nM Compound: mifepristone RU-38486 RU-486	In vitro antagonist potency in transactivation assay in CV-1 cells expressing androgen receptor In vitro antagonist potency in transactivation assay in CV-1 cells expressing androgen receptor	[PMID: 11150172]
CV-1	IC₅₀	5 nM Compound: RU-486 (Mifepristone)	Antagonistic activity against human androgen receptor (hAR) in co-transfected CV-1 cells. Antagonistic activity against human androgen receptor (hAR) in co-transfected CV-1 cells.	[PMID: 9484511]
CV-1	IC₅₀	812 nM Compound: RU-486	Antagonist activity at human ERbeta expressed in african green monkey CV1 cells co-transfected with ERE-MMTV-Luc by luciferase reporter gene assay Antagonist activity at human ERbeta expressed in african green monkey CV1 cells co-transfected with ERE-MMTV-Luc by luciferase reporter gene assay	[PMID: 20510622]
HCC1937	IC₅₀	>20 μM Compound: 1	Antiproliferative activity against human HCC1937 cells after 48 hrs by SRB assay Antiproliferative activity against human HCC1937 cells after 48 hrs by SRB assay	[PMID: 29407962]
HEK293	IC₅₀	0.298 nM Compound: MIF	Antagonist activity against glucocorticoid receptor (unknown origin) expressed in HEK293 cells by GRE-dependent luciferase reporter gene assay Antagonist activity against glucocorticoid receptor (unknown origin) expressed in HEK293 cells by GRE-dependent luciferase reporter gene assay	[PMID: 26218343]
HeLa	EC₅₀	2 nM Compound: RU-486 (Mifepristone)	Effective concentration against inhibition of Dexamethasone induced glucocorticoid receptor transactivation of mouse mammary tumor virus luciferase gene in HeLa cells Effective concentration against inhibition of Dexamethasone induced glucocorticoid receptor transactivation of mouse mammary tumor virus luciferase gene in HeLa cells	[PMID: 16112571]
Hepatocyte	IC₅₀	0.27 μM Compound: 1	Inhibition of dexamethasone-induced glucocorticoid receptor mediated tyrosine aminotransferase in rat hepatocytes Inhibition of dexamethasone-induced glucocorticoid receptor mediated tyrosine aminotransferase in rat hepatocytes	[PMID: 15261265]
Hepatocyte	IC₅₀	0.27 μM Compound: RU-486 (Mifepristone)	Inhibition of dexamethasone-induced GR-mediated tyrosine amino transferase activity in rat hepatocytes Inhibition of dexamethasone-induced GR-mediated tyrosine amino transferase activity in rat hepatocytes	[PMID: 15261266]
Hepatocyte	IC₅₀	0.41 μM Compound: 1 Mifepristone - RU-486	Inhibition of prednisilone-induced tyrosine aminotransferase (TAT) activity in rat hepatocytes Inhibition of prednisilone-induced tyrosine aminotransferase (TAT) activity in rat hepatocytes	[PMID: 12824023]
K562/R7	IC₅₀	0.9 μM Compound: RU486	Potentiation of doxorubicin-induced cytotoxicity against doxorubicin-resistant human K562/R7 cells assessed as doxorubicin IC50 at 1 uM after 72 hrs by MTT assay Potentiation of doxorubicin-induced cytotoxicity against doxorubicin-resistant human K562/R7 cells assessed as doxorubicin IC50 at 1 uM after 72 hrs by MTT assay	[PMID: 25634041]
LNCaP	EC₅₀	11.9 nM Compound: 1	Agonist activity at human androgen receptor in human LNCAP cells harboring firefly luciferase gene after 20 hrs by One-Glo luciferase reporter gene assay Agonist activity at human androgen receptor in human LNCAP cells harboring firefly luciferase gene after 20 hrs by One-Glo luciferase reporter gene assay	[PMID: 31274313]
MCF7	IC₅₀	24.03 μM Compound: Mifepristone	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability after 72 hrs by CCK-8 assay	[PMID: 33461148]
NIH3T3	IC₅₀	2.2 nM Compound: mifepristone RU-38486 RU-486	In vitro antagonist potency in transactivation assay in NIH3T3 cells expressing glucocorticoid receptor In vitro antagonist potency in transactivation assay in NIH3T3 cells expressing glucocorticoid receptor	[PMID: 11150172]
SUM149PT	IC₅₀	15 μM Compound: 1	Antiproliferative activity against human SUM149PT cells after 48 hrs by SRB assay Antiproliferative activity against human SUM149PT cells after 48 hrs by SRB assay	[PMID: 29407962]
T47D	IC₅₀	0.045 nM Compound: 1, RU-486	Antagonist activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity after 48 hrs Antagonist activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity after 48 hrs	[PMID: 19216549]
T47D	IC₅₀	0.05 nM Compound: 10	Antiprogestagenic activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity Antiprogestagenic activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity	[PMID: 20149664]
T47D	IC₅₀	0.054 nM Compound: 1, mifepristone,RU-486	Antagonist activity at progesterone receptor expressed in human T47D cells assessed as inhibition of promegestone-induced alkaline phosphatase activity Antagonist activity at progesterone receptor expressed in human T47D cells assessed as inhibition of promegestone-induced alkaline phosphatase activity	[PMID: 17855092]
T47D	IC₅₀	0.1 nM Compound: 2	Progesterone receptor antagonist activity based on its ability to block progesterone induced alkaline phosphatase in the human breast cancer cell line T47D Progesterone receptor antagonist activity based on its ability to block progesterone induced alkaline phosphatase in the human breast cancer cell line T47D	[PMID: 12419390]
T47D	IC₅₀	0.13 nM Compound: 1	Antagonist activity against progesterone receptor (PR) in an alkaline phosphatase assay in the T47D human breast carcinoma cell line Antagonist activity against progesterone receptor (PR) in an alkaline phosphatase assay in the T47D human breast carcinoma cell line	[PMID: 12238914]
T47D	IC₅₀	0.2 nM Compound: 1, mifepristone	Inhibition of progesterone receptor mediated progesterone-induced alkaline phosphatase activity in human T47D cells Inhibition of progesterone receptor mediated progesterone-induced alkaline phosphatase activity in human T47D cells	[PMID: 18504132]
T47D	IC₅₀	0.2 nM Compound: 2	Antagonist activity at progesterone receptor assessed as progesterone-induced alkaline phosphatase activity in human T47D cells Antagonist activity at progesterone receptor assessed as progesterone-induced alkaline phosphatase activity in human T47D cells	[PMID: 18722119]
T47D	IC₅₀	0.2 nM Compound: 2	Antagonist activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity Antagonist activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity	[PMID: 20638844]
T47D	IC₅₀	0.2 nM Compound: 3, mifepristone	Antagonist activity at human PR expressed in human T47D cells assessed as inhibition of progesterone induced alkaline phosphatase Antagonist activity at human PR expressed in human T47D cells assessed as inhibition of progesterone induced alkaline phosphatase	[PMID: 18318463]
T47D	IC₅₀	0.2 nM Compound: Mifepristone	Inhibitory concentration against progesterone stimulated alkaline phosphatase activity in T47D human breast carcinoma cell line Inhibitory concentration against progesterone stimulated alkaline phosphatase activity in T47D human breast carcinoma cell line	[PMID: 11591515]
T47D	IC₅₀	0.2 nM Compound: Mifepristone RU-486	Antagonistic activity against Progesterone receptor (PR) in transcriptional activation assay in human T47D breast carcinoma cell line Antagonistic activity against Progesterone receptor (PR) in transcriptional activation assay in human T47D breast carcinoma cell line	[PMID: 11859003]
T47D	IC₅₀	0.6 nM Compound: 3, mifepristone	Displacement of [3H]R5020 from human PR in human T47D cells by whole cell assay Displacement of [3H]R5020 from human PR in human T47D cells by whole cell assay	[PMID: 18318463]
T47D	IC₅₀	0.7 nM Compound: Mif (Mifepristone)	Displacement of [3H]progesterone at progesterone receptor of T47D cells Displacement of [3H]progesterone at progesterone receptor of T47D cells	[PMID: 15081005]
T47D	IC₅₀	1.4 nM Compound: Mifepristone	Antagonist activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity Antagonist activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity	[PMID: 17169557]
T47D	IC₅₀	1.4 nM Compound: Mifepristone	Antagonist activity at human progesterone receptor assessed as inhibition of alkaline phosphatase activity in human T47D cells Antagonist activity at human progesterone receptor assessed as inhibition of alkaline phosphatase activity in human T47D cells	[PMID: 17317167]
T47D	IC₅₀	1.4 nM Compound: Mifepristone	Antagonist activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity Antagonist activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity	[PMID: 19217285]
T47D	IC₅₀	3.3 nM Compound: Mifepristone	Inhibition of human progesterone receptor activation in T47D human breast cancer cell. Inhibition of human progesterone receptor activation in T47D human breast cancer cell.	[PMID: 12781198]

In Vitro

The discovery of the first competitive progesterone antagonist, Mifepristone, has stimulated an intense search for more potent and more selective antiprogestins^[1]. Cell growth is evaluated after 4 days of exposure to Mifepristone at 10 μM, a concentration close to the plasma concentration achievable in humans. The antiproliferative effect of NSC 119875 is potentiated when administered in combination with Mifepristone in HeLa cells. The IC₅₀ of NSC 119875 in combination with Mifepristone is lower (14.2 μM) than that of NSC 119875 alone (34.2 μM) in HeLa cells with an approximately 2.5-fold difference. After treatment with Mifepristone, the accumulation of intracellular NSC 119875 in HeLa cells is 2-fold greater, representing a significant difference (p=0.009), compare with NSC 119875 alone from 0.79 to 1.52 μg/mg of protein^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (232.78 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3278 mL	11.6390 mL	23.2780 mL
5 mM	0.4656 mL	2.3278 mL	4.6556 mL
10 mM	0.2328 mL	1.1639 mL	2.3278 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 10 mg/mL (23.28 mM); Suspended solution; Need ultrasonic

Pureté et documentation

Purity: 99.88%

Fiche technique (283 KB) SDS (393 KB)

COA (252 KB) HNMR (277 KB) RP-HPLC (257 KB) LCMS (330 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Jiang W, et al. New progesterone receptor antagonists: phosphorus-containing 11beta-aryl-substituted steroids. Bioorg Med Chem. 2006 Oct 1;14(19):6726-32. [Content Brief]

[2]. Jurado R, et al. NSC 119875 cytotoxicity is increased by mifepristone in cervical carcinoma: an in vitro and in vivo study. Oncol Rep. 2009 Nov;22(5):1237-45. [Content Brief]

[3]. Sharrett-Field L, et al. Mifepristone Pretreatment Reduces Ethanol Withdrawal Severity In Vivo. Alcohol Clin Exp Res. 2013 Aug;37(8):1417-23. [Content Brief]

[4]. Yuehua You, et al. Progesterone Promotes Endothelial Nitric Oxide Synthase Expression Through Enhancing Nuclear Progesterone receptor-SP1 Formation. Am J Physiol Heart Circ Physiol. 2020 Jul 3. [Content Brief]

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