Gw4064 synthesis
WebMay 1, 2014 · GW4064 induces FXR-independent cell death in MCF-7 and HEK cells. A, MCF-7 or HEK cells were plated in 96-well plates (10 000 cells/well) and were … WebBile acid synthesis, transport, and bacterial metabolism Bile acid synthesis. Bile acids can be divided into primary BAs containing cholic acid (CA) and chenodeoxycholic acid (CDCA) and secondary BAs including deoxycholic acid (DCA) and lithocholic acid (LCA). ... GW4064, a specific FXR agonist with no hepatorenal toxicity, ...
Gw4064 synthesis
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WebGW4064 stimulates autophagy in MCF-7 cells. 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 … WebGW4064 is a potent, orally-available, non-steroidal, isoxazole-based agonist of FXR with an EC50 of 15 nM. In a Fisher rat model, GW4064 was found to GW4064, GW-4064, GW …
WebGW4064 is a FXR agonist. There is no activity of GW4064 at other nuclear receptors at concentrations up to 1 μM. Treatment of differentiated 3T3-L1 adipocytes with the FXR … WebWhile oral administration of FXR agonist GW4064 was found to exacerbate weight gain, glucose intolerance and dyslipidemia ... P. R. China), and reverse transcribed to first-strand cDNA using an iScript™ cDNA synthesis kit (Bio-Rad, CA, USA). Then, an UltraSYBR Mixture kit (Thermo Scientific, USA) was used for qPCR analysis on an Applied ...
WebApr 8, 2016 · In this paper, a three level in silico approach was applied to investigate some important structural and physicochemical aspects of a series of anthranilic acid derivatives (AAD) newly identified as potent partial farnesoid X receptor (FXR) agonists. Initially, both two and three-dimensional quantitative structure activity relationship (2D- and 3D-QSAR) … WebGW4064 is a potent (EC50 = 15 nM), non-steroidal agonist of the orphan nuclear receptor FXR. It shows no activity on other nuclear receptors including RAR up to 1 mM. This is an important tool for the study of the involvment of FXR in a variety of biological activities. ... Chemical Synthesis, Chromatography, Analytical and many others. Contact ...
WebJul 29, 2024 · Mortality associated with liver disease has been observed in patients with short bowel syndrome (SBS); however, its mechanism remains unclear, but bile acid (BA) dysmetabolism has been proposed as a possible cause. The farnesoid X receptor (FXR) is the key regulator of BA synthesis. Here, we showed that, in a rat model of short bowel …
WebDownload scientific diagram CDCA and GW4064 increased FGF19 and repressed CYP7A1 mRNA expression in primary human hepatocytes. Primary human hepatocytes were treated with CDCA (50 M) or GW4064 ... how to make head smaller in robloxWebDec 15, 2024 · With this background, a series of isoflavone analogs of GW4064 were designed, synthesized and evaluated the lipid-lowering activity of analogs. As a result, … how to make headset work on pcWebAug 1, 2024 · GW4064 increased the reabsorption of conjugated BAs by inducing apical sodium-dependent bile salt transporter expression in the ileum. Concomitantly, FXR … ms office 2007 tutorialsWebMar 28, 2024 · FXR agonist GW4064 improves liver and intestinal pathology and alters bile acid metabolism in rats undergoing small intestinal resection. ... Both hepatic and intestinal regulation of BA synthesis was characterized by a blunted hepatic FXR activation response. The mRNA expression levels of cholesterol 7a-hydroxylase (CYP7A1), sterol … ms office 2007 product key for windows 7WebJan 5, 2016 · Moreover, the BrdU assay of DNA synthesis supported that GW4064 or CDCA treatment markedly promoted the proliferation of HepG2 cells . FXR antagonist (Z)-Guggulsterone (GS ... ms office 2007 product keysWebJan 15, 2015 · In summary, several novel heterocyclic analogs of GW4064 were designed, synthesized and assayed as FXR agonists. The more active analogs, such as 26, 27, 32 and 33, maintain a putative H-bond acceptor, placed strategically in the ring. These analogs are valuable in designing subsequent analogs, potentially in combination with novel … ms office 2007 pro keyWebDec 15, 2024 · A series of isoflavone analogs of GW4064 have been designed and synthesized. • The most potent compound 15d displayed lipid accumulation inhibitory activities through FXR.. 15d exhibited less toxicity than GW4064 in HepG2 cells.. 15d fitted well in the binding pocket of FXR. ms office 2007 words