计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
Moligand™ 级 ,适用于对基线干扰要求严格的色谱和分析工作流程。
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
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在色谱分析、有机合成和交叉偶联反应领域已被 1 篇同行评审文献引用。
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%
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| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
| 分析证书 | G407795 |