Vaborbactam是一种环状硼酸药效团β-内酰胺酶抑制剂。
Description | Vaborbactam is a cyclic boronic acid pharmacophore β-lactamase inhibitor. | ||||||||||||||||
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In Vitro | Vaborbactam is a broad spectrum of inhibition of β-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 μg/mL, and maximum potentiation is achieved with fixed concentrations of ≥8 μg/mL of the inhibitor (≥96.5% of isolates are inhibited at ≤2 μg/mL of meropenem-vaborbactam). Meropenem-vaborbactam with a fixed concentration of 8 μg/mL of the inhibitor (MIC50, ≤0.06 μg/mL for all organisms) inhibits 93.7% of the CPE isolates displaying elevated meropenem MICs at ≤1 μg/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]. | ||||||||||||||||
Solvent & Solubility | In Vitro: H2O : 30 mg/mL (100.96 mM; Need ultrasonic and warming) Preparing Stock Solutions
* Please refer to the solubility information to select the appropriate solvent. | ||||||||||||||||
References |
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