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GW4064, 法尼类固醇 X 受体激动剂

FXR Agonists
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货号 (SKU) 包装规格 是否现货 价格 数量
G407795-1ml
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Compound libraries (12333)

基本描述

英文别名 Benzoic acid, 3-[2-[2-chloro-4-[[3-(2,6-dichlorophenyl)-5-(1-methylethyl)-4-isoxazolyl]methoxy]phenyl]ethenyl]-
规格或纯度 Moligand™, 10mM in DMSO
英文名称 GW4064
生化机理 GW4064 是法尼类固醇 X 受体 (FXR) 的激动剂,在 CV1 细胞系中的 EC50 为 65 nM,在浓度高达 1 μM 时对其他核受体没有活性。GW4064 可刺激 MCF-7 细胞的自噬。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 激动剂
作用机制 法尼类固醇 X 受体激动剂
产品介绍

GW4064是一种farnesoid X receptor (FXR)激动剂,CV1细胞系中EC50为65 nM。浓度达到1 μM时,对其他核受体没有活性 

应用

研究其保护小鼠肝脏免受脂多糖(LPS)诱导炎症和细胞凋亡影响的能力 

研究其抑制脂多糖(LPS)引起回肠粘膜损伤的能力 

处理回肠外植体

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 t1/2 = 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%

关联靶点(人)

NR1H4 Tclin 胆汁酸受体(Bile acid receptor) (40 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

EC号 631-072-7
分子类型 小分子
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
关联CAS 292047-56-4,1089660-72-9,278779-30-9
MeSH Entry Terms GW 4064;GW-4064;GW4064
分子量 542.84
Reaxy-Rn 10125635
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=10125635&ln=

化学和物理性质

溶解性 Solubility (25°C) In vitro      

安全和危险性(GHS)

WGK Germany 3
个人防护装备 dust mask type N95 (US), Eyeshields, Gloves

质检证书(CoA,COO,BSE/TSE 和分析图谱)

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此产品的引用文献

引用文献

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,  452  (131310).  [PMID:37003002] [10.1016/j.jhazmat.2023.131310]

溶液计算器