AAA-10 formic 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. thetarBSH 和B. longumrBSH 的IC50值分别为 10 nM, 80 nM。
产品描述
AAA-10 formic is an orally active gut bacterial bile salt hydrolases ( BSH ) inhibitor, with IC 50 s of 10 nM, 80 nM against B. theta rBSH and B. longum rBSH, respectively [1].
体外活性
AAA-10 (100 μM; 24 h) formic inhibits BSH activity in bacterial cultures, with IC 50 s of 74 nM, 901 nM for Gram-negative and Gram-positive bacteria, respectively [1]. AAA-10 (20 μM; 2 h) formic significantly inhibits deconjugation of glycochenodeoxycholic acid- d 4 or taurocholic acid- d 4 substrates of human feces [1].
体内活性
AAA-10 (30 mg/kg; orally gavage daily for 5 days) formic 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) formic displays high colonic exposure and low gut permeability [1]. Animal Model: 10-11 weeks old male C57Bl/6J mice [1] Dosage: 30 mg/kg Administration: Orally gavaged once daily for 5 days Result: Decreased the abundances of DCA and LCA in mice feces starting in day 2-5. Displayed high colonic exposure and low gut permeability.
分子式
C26H43FO7S
分子量
518.68
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years