AAA-10 是一种具有口服活性的肠道细菌胆盐水解酶 (BSH) 抑制剂，对B. theta rBSH 和 B. longum rBSH 的 IC50 值分别为 10 nM, 80 nM。
货号:ajcx37230
CAS:N/A
分子式:C25H41FO5S
分子量：472.65
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

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].

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].

[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.