GW4064 - Moligand™, 10mM in DMSO , Agonist of Farnesoid X receptor, CAS No.278779-30-9, Agonist of Farnesoid X receptor

CAS: 278779-30-9 Cat. No.: G407795 Formula: C₂₈H₂₂Cl₃NO₄ Molecular Weight: 542.84 EC Number: 631-072-7

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

Benzoic acid, 3-[2-[2-chloro-4-[[3-(2,6-dichlorophenyl)-5-(1-methylethyl)-4-isoxazolyl]methoxy]phenyl]ethenyl]-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

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%

Specifications

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

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

AGONIST

Mechanism of action

Agonist of Farnesoid X receptor

Names and Identifiers

• Isomeric SMILES: CC(C)C1=C(C(=NO1)C2=C(C=CC=C2Cl)Cl)COC3=CC(=C(C=C3)/C=C/C4=CC(=CC=C4)C(=O)O)Cl
• WGK Germany: 3
• Alternate CAS: 292047-56-4,1089660-72-9,278779-30-9
• MeSH Entry Terms: GW 4064;GW-4064;GW4064
• Molecular Weight: 542.84
• Reaxy-Rn: 10125635
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=10125635&ln=

Associated Targets(Human)

NR1H4 Tclin Bile acid receptor (40 Activities)

Discover Target: NR1H4

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

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro

References

1. Zhiyuan Meng, Sen Yan, Wei Sun, Jin Yan, Miaomiao Teng, Ming Jia, Sinuo Tian, Zhiqiang Zhou, Wentao Zhu.  (2023)  Chlorothalonil induces obesity in mice by regulating host gut microbiota and bile acids metabolism via FXR pathways.  JOURNAL OF HAZARDOUS MATERIALS,      [PMID:37003002] [10.1016/j.jhazmat.2023.131310]