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Glycine-β-muricholic acid (GβMCA) is an intestine-selective antagonist of the farnesoid X receptor (FXR) and the glycine-conjugated form of the murine-specific primary bile acid β-muricholic acid .[1] [2]  It inhibits expression of the FXR target genes Shp and Fgf15 induced by the FXR ligands chenodeoxycholic acid and GW 4064 in Caco-2 cells when used at a concentration of 100 μM. GβMCA is resistant 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 not liver, 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/db mice. It also prevents weight gain, reduces blood glucose levels, and increases insulin sensitivity as well as prevents development of cholestasis and necrotic lesions in liver of mice with high-fat diet-induced obesity.

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