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• 产品描述： Vaborbactam (RPX7009) is a cyclic boronic acid pharmacophore β-lactamase inhibitor.

• 靶点： Bacterial;Antibacterial

• 体外研究：
  Vaborbactam is a broad spectrum of inhibition of β-lactamases, with particularly potent activity against KPC, CTX-M, SHV, and CMY enzymes. Vaborbactam restores SM 7338 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 SM 7338-vaborbactam). SM 7338-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 SM 7338 MICs at ≤1 μg/mL. By forming a reversible dative bond with the blactamase, vaborbactam acts as a competitive inhibitor and is not hydrolyzed by the b-lactamase

• 体内研究：
  Vaborbactam is well tolerated and has a half-life of 1.23 h, and steadystate volume of distribution of 21.0 L in subjects

• 参考文献：
  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 SM 7338 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. Drugs. 2017 Apr;77(6):615-628.

• 溶解性： Soluble  in  H2O

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.365 ml	16.827 ml	33.655 ml
  5 mM	0.673 ml	3.365 ml	6.731 ml
  10 mM	0.337 ml	1.683 ml	3.365 ml
  50 mM	0.067 ml	0.337 ml	0.673 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *