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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].
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $1,520 | 10-14 weeks | |
50 mg | $1,980 | 10-14 weeks | |
100 mg | $2,500 | 10-14 weeks |
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) at 10 μM significantly impedes P. aeruginosa biofilm formation by 74%, concurrently reducing carbohydrate and protein content by 39% and 72%, respectively, and markedly curtails rhamnolipid synthesis at both 10 and 100 μM. A 24-hour exposure to 0-10 μM levels notably suppresses rhlA gene expression in biofilm cells. Thus, this compound effectively obstructs P. aeruginosa biofilms and virulence factor production by down-regulating rhlA expression in P. aeruginosa. |
In vivo | Larvae administered with P. aeruginosa began experiencing mortality within the initial incubation phase, resulting in a 70% mortality rate by the conclusion of the 20-day period. Treatment with RhlR antagonist 1 (0-10 μM) significantly enhanced survival, with about 80% of larvae surviving by the period's end. Moreover, larvae inoculated with rhlR mutants of P. aeruginosa exhibited a 90% survival rate after 20 days [1]. |
Molecular Weight | 208.2 |
Formula | C12H10F2O |
Storage | Shipping with blue ice. |
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