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(Synonyms: RPX 7009) Catalog No.: GC19369

Vaborbactam is a cyclic boronic acid pharmacophore β-lactamase inhibitor.

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Vaborbactam Chemical Structure

Cas No.:1360457-46-0

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10mM (in 1mL Water)
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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].

[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.

Chemical Properties

Cas No. 1360457-46-0 SDF
Synonyms RPX 7009
Canonical SMILES O=C(O)C[C@@H]1CC[C@H](NC(CC2=CC=CS2)=O)B(O)O1
Formula C12H16BNO5S M.Wt 297.14
Solubility Water : 5.26 mg/mL (17.70 mM) Storage 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.Stock solution can be stored below -20℃ for several months.
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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Average Rating: 5 ★★★★★ (Based on Reviews and 23 reference(s) in Google Scholar.)

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