Gut restricted-7 (GR-7) is a potent, covalent and orally active pan-bile salt hydrolase (BSH) inhibitor. Gut restricted-7 decreases gut bacterial BSHs and decreases deconjugated bile acid levels in feces of mice[1].
BSH Inhibitor Gut restricted-7 (GR-7) (60 μM) does not affect epithelial barrier integrity of Caco-2 cells, suggesting that this compound is relatively nontoxic. Gut restricted-7 also does not affect microbial biomass[1].
The C57BL/6 mice fed with either powdered chow containing 0.09% Gut restricted-7 (GR-7) (w/w) for 1 d day or powdered chow alone. Gut restricted-7 significant inhibits the BSH activity in the feces of inhibitortreated mice 8 h postdiet change. 20picomol/mg wet mass (~20 μM) of Gut restricted-7 in cecal contents is detected[1].
[1]. Adhikari AA, et al. Development of a covalent inhibitor of gut bacterial bile salt hydrolases. Nat Chem Biol. 2020 Mar;16(3):318-326.