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RhlR antagonist 1

CAS No. :

MCE 站：RhlR antagonist 1

产品活性：RhlR antagonist 1 是一种有效的 RhlR 拮抗剂，IC₅₀ 为 26 μM。RhlR antagonist 1 对 LasR 和 PqsR 表现出选择性的 RhlR 拮抗作用，在静态和动态环境下对生物膜的形成有较强的抑制作用，并能减少绿脓杆菌毒力因子的产生，如鼠李糖脂和绿脓杆菌素等。RhlR antagonist 1 可用于开发 QS 调节分子来控制铜绿假单胞菌感染。

研究领域：Anti-infection

作用靶点：Bacterial

In Vitro: RhlR antagonist 1 (compound 30) (10 μM) inhibits P. aeruginosa biofilm formation by 74% ａnd decreases the amount of carbohydrate ａnd protein by 39 ａnd 72%, respectively. RhlR antagonist 1 reduces significantly rhamnolipid production by P. aeruginosa at 10 ａnd 100 μM concentrations. RhlR antagonist 1 (0-10 μM; 24 hours) down-regulates rhlA expression of biofilm cells. RhlR antagonist 1 could inhibit P. aeruginosa biofilm formation ａnd virulence factor production by down-regulating the rhlA expression of PP. aeruginosa.

In Vivo: Larvae injected with P. aeruginosa started to die in initial incubation time ａnd 70% of them died at the end of the 20-day incubation period. The survival rate of RhlR antagonist 1 (0-10 μM)-treated larvae is greatly improved, with approximately 80% larvae surviving at the end of the incubation period. In addition, larvae injected with rhlR mutants of P. aeruginosa shows a 90% survival rate after 20 days.

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