Mifepristone (RU486) - Moligand™, 10mM in DMSO , Progesterone receptor antagonist, CAS No.84371-65-3, Progesterone receptor antagonist

CAS: 84371-65-3 Cat. No.: M408467 Formula: C₂₉H₃₅NO₂ Peso molecolare: 429.59 Numero EC: 617-559-7

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

C-1073, RU 38486, Mifegyne | (11β,​17β)​-11-​[4-​(dimethylamino)​phenyl]​-​17-​hydroxy-​17-​(1-​propyn-​1-​yl)​-estra-​4,​9-​dien-​3-​one

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Panoramica

Information

Mifepristone (RU486, C-1073, RU 38486, Mifegyne) is a remarkably active antagonist ofprogesterone receptorandglucocorticoid receptorwithIC50of 0.2 nM and 2.6 nM, respectively. Mifepristone promotes cellautophagyandapoptosis, decreasesBcl-2level and increa
In vitro

Mifepristone inhibit corticoid-induced transcription from a glucocorticoid response element (GRE)-linked luciferase reporter gene in the human lung carcinoma cell line A549. Moreover, Mifepristone also blocks progesterone induction of alkaline phosphatase activity in the human breast cancer cell line T47D. Mifepristone inhibits ovarian cancer cell growth of SK-OV-3 and OV2008 with IC50 of 6.25 μM and 6.91 μM, respectively. A recent study shows that Mifepristone induces caspase-1 over expression both in differentiated and undifferentiated caspase-1-embryonic stem cells.

In vivo

Mifepristone can impair the growth of SK-OV-3 tumors in immunosuppressed mice at 0.5 mg/day and 1 mg/day. Mifepristone inhibits the prostate weight significantly in the highest doses in vivo, and inhibits growth of the prostate gland produced by dihydrotestosterone (DHT) to a greater extent than the induction of atrophy and cell death in rats.
Cell Data

cell lines：

Concentrations：0-20 μM

Incubation Time：24 hours

Powder Purity:≥99%

Specifications

Sinonimi

C-1073, RU 38486, Mifegyne | (11β,​17β)​-11-​[4-​(dimethylamino)​phenyl]​-​17-​hydroxy-​17-​(1-​propyn-​1-​yl)​-estra-​4,​9-​dien-​3-​one

Specifiche e purezza

Moligand™, 10mM in DMSO

Meccanismi biochimici e fisiologici

Mifepristone (RU486, C-1073, RU 38486, Mifegyne) is a remarkably active antagonist of progesterone receptor and glucocorticoid receptor with IC50 of 0.2 nM and 2.6 nM, respectively. Mifepristone promotes cell autophagy and apoptosis, decreases Bcl-2 level

Condizioni di conservazione di stoccaggio

Store at -80°C

Spedito in

Dry ice packs + Cold packs

Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.

Grado

Moligand™

Tipo di azione

AGONIST, ANTAGONIST

Meccanismo d'azione

Progesterone receptor antagonist

Proprietà del prodotto

ALogP

3.8

Nomi e identificatori

Isomeri SMILES

CC#C[C@@]1(CC[C@@H]2[C@@]1(C[C@@H](C3=C4CCC(=O)C=C4CC[C@@H]23)C5=CC=C(C=C5)N(C)C)C)O

WGK Germania

3

RTECS

KG2955000

Peso molecolare

429.59

Reaxy-Rn

24984138

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=24984138&ln=

Obiettivi associati (umani)

NR3C1 Tclin Glucocorticoid receptor (67 Activities)

Discover Target: NR3C1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PGR Tclin Progesterone receptor (57 Activities)

Discover Target: PGR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

NR1I2 Tchem Nuclear receptor subfamily 1 group I member 2 (1 Activities)

Discover Target: NR1I2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AR Tclin Androgen receptor (27 Activities)

Discover Target: AR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Proprietà chimiche e fisiche

• Solubilità: Solubility (25°C) In vitro DMSO: 30 mg/mL (197.13 mM); Water: Insoluble; Ethanol: Insoluble
• Rotazione specifica [α]: 141° (C=0.5,CHCl3)
• Punto di fusione (°C): 195 °C