|Vaborbactam 目录号 GC19369|
Sample solution is provided at 25 µL, 10mM.
|Cas No.||1360457-46-0||SDF||Download SDF|
|溶解度||H2O : 5.26 mg/mL (17.70 mM)||储存条件||Store at -20°C|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.|
|Shipping Condition||Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
Vaborbactam is a cyclic boronic acid pharmacophore β-lactamase inhibitor.
Vaborbactam is a broad spectrum of inhibition of β-lactamases, with particularly potent activity against KPC, CTX-M, SHV, and CMY enzymes. 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. By forming a reversible dative bond with the blactamase, vaborbactam acts as a competitive inhibitor and is not hydrolyzed by the b-lactamase.
Vaborbactam is well tolerated and has a half-life of 1.23 h, and steadystate volume of distribution of 21.0 L in subjects.
. Hecker SJ, et al. Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. J Med Chem. 2015 May 14;58(9):3682-92.
. Castanheira M, et al. Effect of the β-Lactamase Inhibitor Vaborbactam Combined with Meropenem against Serine Carbapenemase-Producing Enterobacteriaceae. Antimicrob Agents Chemother. 2016 Aug 22;60(9):5454-8.
. Wong D, et al. Novel Beta-Lactamase Inhibitors: Unlocking Their Potential in Therapy.