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 분자식: C₂₈H₂₂Cl₃NO₄ 분자량: 542.84 EC 번호: 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

개요

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

동의어

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

사양 및 순도

Moligand™, 10mM in DMSO

생화학 및 생리적 메커니즘

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.

보관 조건

Store at -80°C

배송

Dry ice packs + Cold packs

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등급

Moligand™

작업 유형

AGONIST

작동 메커니즘

Agonist of Farnesoid X receptor

이름과 식별자

• 이성체 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 독일: 3
• 대체 CAS: 292047-56-4,1089660-72-9,278779-30-9
• MeSH 용어: GW 4064;GW-4064;GW4064
• 분자량: 542.84
• Reaxy-Rn: 10125635
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=10125635&ln=

관련 대상(인간)

NR1H4 Tclin Bile acid receptor (40 Activities)

Discover Target: NR1H4

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

화학 및 물리적 특성

• 용해성: Solubility (25°C) In vitro

참고 문헌

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]

자주 묻는 질문

What is Moligand??

Moligand? is one of Aladdin Scientific's premium product lines, formulated for high-purity applications across multiple workflows. Compared to standard grades in the same workflow, Moligand? products typically offer tighter specifications, more rigorous QC, and stronger lot-to-lot consistency.

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 278779-30-9, the molecular formula is C28H22Cl3NO4, and the molecular weight is 542.84 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.