Vaborbactam

1360457-46-0

C12H16BNO5S

H2O : 5.26 mg/mL (17.70 mM; Need ultrasonic)

Anti-infection

Vaborbactam is a cyclic boronic acid pharmacophore beta-lactamase inhibitor. In Vitro: Vaborbactam is a broad spectrum of inhibition of beta-lactamases, with particularly potent activity against KPC, CTX-M, SHV, and CMY enzymes^[1]. Vaborbactam restores meropenem activity for 72.7 to 98.1% of CPE isolates at <=2 ug/mL, and maximum potentiation is achieved with fixed concentrations of >=8 ug/mL of the inhibitor (>=96.5% of isolates are inhibited at <=2 ug/mL of meropenem-vaborbactam). Meropenem-vaborbactam with a fixed concentration of 8 ug/mL of the inhibitor (MIC50, <=0.06 ug/mL for all organisms) inhibits 93.7% of the CPE isolates displaying elevated meropenem MICs at <=1 ug/mL^[2]. By forming a reversible dative bond with the blactamase, vaborbactam acts as a competitive inhibitor and is not hydrolyzed by the b-lactamase^[3]. In Vivo: Vaborbactam is well tolerated and has a half-life of 1.23 h, and steadystate volume of distribution of 21.0 L in subjects^[3].