Glycine-β-muricholic Acid (Synonyms: Gly-MCA, GβMCA) |
カタログ番号GC40911 |
グリシン-β-胆汁酸であるムリコール酸は、代謝性疾患の治療の候補となる可能性のある強力なクロテンの腸選択的経口生理活性ファルネソイド X 受容体 (FXR) 阻害剤です。
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Cas No.: 66225-78-3
Sample solution is provided at 25 µL, 10mM.
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.
Reference:
[1]. Jiang, C., Xie, C., Lv, Y., et al. Intestine-selective farnesoid X receptor inhibition improves obesity-related metabolic dysfunction. Nat. Commun. 6, 10166 (2015).
[2]. Wahlström, A., Sayin, S.I., Marschall, H.-I., et al. Intestinal crosstalk between bile acids and microbiota and its impact on host metabolism. Cell Metab. 24(1), 41-50 (2016).
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