PAbetaN (dihydrochloride)

100929-99-5

C25H32Cl2N6O2

DMSO : >= 100 mg/mL (192.50 mM); H2O : 14.29 mg/mL (27.51 mM; Need ultrasonic)

Anti-infection

PAbetaN dihydrochloride (MC-207110 dihydrochloride) is an efflux pump inhibitor. In Vitro: PAbetaN increases the susceptibilities of the three pump-overexpressing mutants of P. aeruginosa to levofloxacin 64-fold. PAbetaN also potentiates the activity of levofloxacin against strain PAM2391 containing plasmid pAGH97 with the mexXY genes and against wild-type strain PAM1020. PAbetaN has an effect on susceptibilities to other antibiotics that are substrates of efflux pumps. PAbetaN increases levels of accumulation of efflux pump substrates inside the cell. It enhances the activity of levofloxacin against clinical isolates of P. aeruginosa^[1]. PAbetaN reduces the MICs in nine ciprofloxacin-resistant isolates, and in four of these, PAbetaN increases the susceptibility by twofold. Moreover, PAbetaN restores ciprofloxacin susceptibility in five of the ciprofloxacin-resistant isolates. In addition, clear effects of NMP on the ciprofloxacin MICs are seen for 20 of these ciprofloxacin-resistant isolates^[2]. PAbetaN permeabilizes bacterial membranes in a concentration-dependent manner at levels below those typically used in combination studies, and this additional mode of action should be considered when using PAbetaN as a control for efflux studies^[3].