An intestine-selective FXR antagonist; glycine-conjugated form of β-muricholic acid; inhibits chenodeoxycholic acid- and GW 4064-induced expression of the FXR target genes Shp and Fgf15 at 100 μM; resistant to hydrolysis by fecal BSH isolated from gut microbiota; decreases Shp and Fgf15 mRNA expression in ileum

Glycine-β-muricholic Acid – 5 mg

Brand:
Cayman
CAS:
66225-78-3
Storage:
-20
UN-No:
Non-Hazardous - /

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 (Item No. 20287).{36870,45190} It inhibits expression of the 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 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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SKU: 9003230 - 5 mg Category:

Description

An intestine-selective FXR antagonist; glycine-conjugated form of β-muricholic acid; inhibits chenodeoxycholic acid- and GW 4064-induced expression of the FXR target genes Shp and Fgf15 at 100 μM; resistant to hydrolysis by fecal BSH isolated from gut microbiota; decreases Shp and Fgf15 mRNA expression in ileum, but not liver, and reduces ceramide levels and expression of various ceramide synthesis-related genes in ileum of mice with high-fat diet-induced obesity and db/db mice at 10 mg/kg; 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

Formal name: N-[(3α,5β,6β,7β)-3,6,7-trihydroxy-24-oxocholan-24-yl]-glycine

Synonyms:  Gly-MCA|GβMCA

Molecular weight: 465.6

CAS: 66225-78-3

Purity: ≥95%

Formulation: A crystalline solid

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