| Bioactivity | AAA-10 is an orally active gut bacterial bile salt hydrolases (BSH) inhibitor, with IC50s of 10 nM, 80 nM against B. theta rBSH and B. longum rBSH respectively[1]. | ||||||||||||
| Target | IC50: 10 nM (B. theta rBSH), 80 nM (B. longum rBSH) | ||||||||||||
| Invitro | AAA-10 (100 μM; 24 h) inhibits BSH activity in bacterial cultures, with IC50s of 74 nM, 901 nM for Gram-negative and Gram-positive bacteria, respectively[1]. AAA-10 (20 μM; 2 h) significantly inhibits deconjugation of glycochenodeoxycholic acid-d4 or taurocholic acid-d4 substrates of human feces[1]. | ||||||||||||
| In Vivo | AAA-10 (30 mg/kg; orally gavage daily for 5 days) decreases the abundances of deoxycholic acid (DCA) and lithocholic acid (LCA) in mice feces starting in day 2-5[1].AAA-10 (30 mg/kg) displays high colonic exposure and low gut permeability[1]. Animal Model: | ||||||||||||
| Name | AAA-10 | ||||||||||||
| Formula | C25H41FO5S | ||||||||||||
| Molar Mass | 472.65 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Adhikari AA, et al. A Gut-Restricted Lithocholic Acid Analog as an Inhibitor of Gut Bacterial Bile Salt Hydrolases. ACS Chem Biol. 2021;16(8):1401-1412. |