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Vaborbactam 目录号 GC19369

规格 价格 库存 购买数量
10 mM * 1 mL in Water
¥3,236.00
现货
1mg
¥990.00
现货
5mg
¥3,150.00
现货
10mg
¥4,500.00
现货
50mg
¥13,500.00
现货
100mg
¥18,900.00
现货

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Sample solution is provided at 25 µL, 10mM.

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Chemical Properties

Cas No. 1360457-46-0 SDF Download SDF
别名 N/A
化学名 N/A
Canonical SMILES O=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 H2O : 5.26 mg/mL (17.70 mM; Need ultrasonic) 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
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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.