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BSH-IN-1 is a potent and covalent inhibitor of gut bacterial recombinant bile salt hydrolases (BSHs) with IC50s of 108 nM and 427 nM for B. longum BSH (Gram positive) and B. theta BSH (Gram negative), respectively[1].

BSH-IN-1 (Compound 7) also inhibits BSH activity in growing cultures of Gram-negative (B. theta VPI-5482, Bacteroides fragilis ATCC 25285, and Bacteroides vulgatus ATCC 8482) and Gram-positive (Lactobacillus plantarum WCFS1, C. perfringens ATCC 13124, and Bifidobacterium adolescentis L2-32) bacteria. BSH-IN-1 (Compound 7) also is a potent BSH inhibitor in growing bacterial cultures with IC50s of 237 nM and 1070 nM for B. adolescentis (Gram positive) and B. theta (Gram negative), respectively[1].

BSH-IN-1 (Compound 7; 10 mg/kg; a single dose; gavage) inhibits BSH activity in C57BL/6 mice and can be gut-restricted[1]. Animal Model: C57BL/6 mice[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.

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