Farnesoid X receptor (FXR) antagonist. Accumulates in ileum and inhibits FXR signaling exclusively in intestine. Inhibits or reverses high-fat diet-induced and genetic obesity, insulin resistance and hepatic steatosis in mice. Reduces obesity and metaboli
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Product Description
GβMCA is an intestine-selective antagonist of the farnesoid X receptor (FXR) and the glycine-conjugatedform of the murine-specific primary bile acid β-muricholic acid (Item No. 20287).1,2 It inhibits expression ofthe FXR target genes Shp and Fgf15 induced by the FXR ligands chenodeoxycholic acid (Item No. 10011286)and GW 4064 (Item No. 10006611) in Caco-2 cells when used at a concentration of 100 μM. GβMCA isresistant to hydrolysis by fecal bile salt hydrolase (BSH) isolated from gut microbiota, indicating gut stability.Dietary administration of GβMCA (10 mg/kg) decreases Shp and Fgf15 mRNA expression in ileum, but notliver, and reduces ceramide levels and expression of the ceramide synthesis-related genes Sptlc2, Sptlc3,Cers2, Cers4, Degs1, Degs2, Smpd3, and Smpd4 in ileum of mice with high-fat diet-induced obesity and db/dbmice. It also prevents weight gain, reduces blood glucose levels, and increases insulin sensitivity as well asprevents development of cholestasis and necrotic lesions in liver of mice with high-fat diet-induced obesity.
