| Description | RhlR antagonist 1 is a highly effective antagonist of the RhlR protein, showing an IC50 value of 26 μM. It exhibits selective antagonistic activity against RhlR, with minimal effect on LasR and PqsR. RhlR antagonist 1 strongly inhibits biofilm formation in both static and dynamic environments and reduces the production of virulence factors, such as rhamnolipid and pyocyanin, in P. aeruginosa. These characteristics make RhlR antagonist 1 a valuable tool for the development of molecules that modulate quorum sensing and control P. aeruginosa infections [1]. |
| In vitro | RhlR antagonist 1 (compound 30) (10 μM) inhibits P. aeruginosa biofilm formation by 74% and reduces 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 P P. aeruginosa [1]. |
| In vivo | Larvae injected with P. aeruginosa began to die within the initial incubation period, 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 [1]. |
| molecular weight | 208.2 |
| Molecular formula | C12H10F2O |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |