GW4064 - 10mM in DMSO, high purity , CAS No.278779-30-9(DMSO), Agonist of Farnesoid X receptor

Item Number

G407795

• Synonyms: Benzoic acid, 3-[2-[2-chloro-4-[[3-(2,6-dichlorophenyl)-5-(1-methylethyl)-4-isoxazolyl]methoxy]phenyl]ethenyl]-
• Specifications & Purity: Moligand™, 10mM in DMSO
• Biochemical and Physiological Mechanisms: GW4064 is an agonist of farnesoid X receptor (FXR) with EC50 of 65 nM in CV1 cell line and displays no activity at other nuclear receptors at concentrations up to 1 μM. GW4064 stimulates autophagy in MCF-7 cells.
• Storage Temp: Store at -80°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™
• Action Type: AGONIST
• Mechanism of action: Agonist of Farnesoid X receptor

Product Description

Information

GW4064 GW4064 is an agonist of farnesoid X receptor (FXR) with EC50 of 65 nM in CV1 cell line and displays no activity at other nuclear receptors at concentrations up to 1 μM. GW4064 stimulates autophagy in MCF-7 cells.
In vitro

GW 4064 is a full agonist with EC50 values of 80 and 90 nM, respectively, in CV-1 cells transfected with mouse and human FXR expression vectors and an established reporter gene. There is no activity of GW 4064 on other nuclear receptors, including the retinoic acid receptor, at concentrations up to 1 μM. Thus, GW 4064 is a potent and selective nonsteroidal FXR agonist.

In vivo

Pharmacokinetic analysis in rats shows that GW 4064 possesses an oral bioavailability of 10% with a t_1/2 = 3.5 h. Fisher rats are dosed with GW 4064 by oral gavage. After 7 days, a dose-dependent lowering of serum triglycerides is observed in the rats receiving GW 4064, with an ED50 = 20 mg/kg.
Cell Data

cell lines：A2780 cells

Concentrations：

Incubation Time：

Powder Purity:≥99%