GW4064 - CAS 278779-30-9
Catalog number: 278779-30-9
Category: Inhibitor
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GW4064 is a selective non-steroidal agonist of farnesoid X receptor (FXR) with EC50 value of 15 nM.
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1.FXR Primes the Liver for Intestinal FGF15 Signaling by Transient Induction of β-Klotho.
Fu T1, Kim YC1, Byun S1, Kim DH1, Seok S1, Suino-Powell K1, Xu HE1, Kemper B1, Kemper JK1. Mol Endocrinol. 2016 Jan;30(1):92-103. doi: 10.1210/me.2015-1226. Epub 2015 Oct 27.
The bile acid (BA)-sensing nuclear receptor, farnesoid X receptor (FXR), regulates postprandial metabolic responses, including inhibition of BA synthesis, by inducing the intestinal hormone, fibroblast growth factor (FGF)15 (FGF19 in human). In this study, we tested a novel hypothesis that FXR not only induces intestinal FGF15 but also primes the liver for effectively responding to the signal by transcriptional induction of the obligate coreceptor for FGF15, β-Klotho (βKL). Activation of FXR by a synthetic agonist, GW4064, in mice increased occupancy of FXR and its DNA-binding partner, retinoid X receptor-α, at FGF15-signaling component genes, particularly βKL, and induced expression of these genes. Interestingly, mRNA levels of Fgfr4, the FGF15 receptor, were not increased by GW4064, but protein levels increased as a result of βKL-dependent increased protein stability. Both FGF receptor 4 and βKL protein levels were substantially decreased in FXR-knockout (KO) mice, and FGF19 signaling, monitored by phosphorylated ERK, was blunted in FXR-KO mice, FXR-KO mouse hepatocytes, and FXR-down-regulated human hepatocytes.
2.AMPK activation by liquiritigenin inhibited oxidative hepatic injury and mitochondrial dysfunction induced by nutrition deprivation as mediated with induction of farnesoid X receptor.
Jung EH1, Lee JH1,2, Kim SC1, Kim YW3. Eur J Nutr. 2015 Dec 8. [Epub ahead of print]
PURPOSE: Nutrition is indispensable for cell survival and proliferation. Thus, loss of nutrition caused by serum starvation in cells could induce formation of reactive oxygen species (ROS), resulting in cell death. Liquiritigenin (LQ) is an active flavonoid in licorice and plays a role in the liver as a hepatic protectant.
3.Farnesoid X receptor regulates vasoreactivity via Angiotensin II type 2 receptor and the kallikrein-kinin system in vascular endothelial cells.
Zhang R1, Ran H2, Peng L1, Zhang Y1, Shen W1, Sun T1, Cao F1, Chen Y1. Clin Exp Pharmacol Physiol. 2016 Mar;43(3):327-34. doi: 10.1111/1440-1681.12535.
Vascular farnesoid X receptor (FXR) ligands have been shown previously to regulate vascular tension. This study investigated whether FXR activation regulates vasoreactivity via the angiotensin II (Ang II) type 2 receptor (AT2 R) and the kallikrein-kinin system in rat aortic vascular endothelial cells (RAECs). Protein abundances of Ang II type 1 receptor (AT1 R), AT2 R, bradykinin type 1/2 receptor (B1 R, B2 R), small heterodimer partner-1 (SHP-1) and the endothelial and inducible NO synthases (eNOS/iNOS) were analysed by Western blotting. Real-time quantitative polymerase chain reaction was performed to analyse expression of eNOS and iNOS mRNA. Kallikrein activity and bradykinin content were assayed using spectrophotometry and a bradykinin assay kit, respectively. Aortic vasoconstriction and vasodilation were also investigated following FXR activation in the presence or absence of AT2 R and B2 R blockade. It was found that the FXR agonists GW4064 and INT-747, in a dose-dependent manner, increased the protein abundance of AT2 R, B2 R and SHP-1 and decreased that of AT1 R.
4.Hormesis in Cholestatic Liver Disease; Preconditioning with Low Bile Acid Concentrations Protects against Bile Acid-Induced Toxicity.
Verhaag EM1, Buist-Homan M1,2, Koehorst M2, Groen AK2,3, Moshage H1,2, Faber KN1,2. PLoS One. 2016 Mar 7;11(3):e0149782. doi: 10.1371/journal.pone.0149782. eCollection 2016.
INTRODUCTION: Cholestasis is characterized by accumulation of bile acids and inflammation, causing hepatocellular damage. Still, liver damage markers are highest in acute cholestasis and drop when this condition becomes chronic, indicating that hepatocytes adapt towards the hostile environment. This may be explained by a hormetic response in hepatocytes that limits cell death during cholestasis.
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