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Vaborbactam
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Vaborbactam图片
CAS NO:1360457-46-0
包装与价格:
包装价格(元)
10mM (in 1mL Water)电议
1mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Vaborbactam (RPX7009) 是一种环状硼酸药效团 β-内酰胺酶抑制剂。
Cas No.1360457-46-0
别名法硼巴坦,RPX7009
Canonical SMILESO=C(O)C[C@@H]1CC[C@H](NC(CC2=CC=CS2)=O)B(O)O1
分子式C12H16BNO5S
分子量297.14
溶解度Water : 5.26 mg/mL (17.70 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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[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].

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].

References:
[1]. 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.
[2]. 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.
[3]. Wong D, et al. Novel Beta-Lactamase Inhibitors: Unlocking Their Potential in Therapy.