Vaborbactam

Modify Date: 2024-01-02 20:18:06

Vaborbactam Structure
Vaborbactam structure
Common Name Vaborbactam
CAS Number 1360457-46-0 Molecular Weight 297.135
Density 1.4±0.1 g/cm3 Boiling Point N/A
Molecular Formula C12H16BNO5S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Vaborbactam


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

 Names

Name vaborbactam
Synonym More Synonyms

 Vaborbactam Biological Activity

Description Vaborbactam is a cyclic boronic acid pharmacophore β-lactamase inhibitor.
Related Catalog
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].
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.

 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Molecular Formula C12H16BNO5S
Molecular Weight 297.135
Exact Mass 297.084229
Index of Refraction 1.572
Storage condition 2-8℃

 Synonyms

1,2-Oxaborinane-6-acetic acid, 2-hydroxy-3-[[2-(2-thienyl)acetyl]amino]-, (3R,6S)-
{(3R,6S)-2-Hydroxy-3-[(2-thienylacetyl)amino]-1,2-oxaborinan-6-yl}acetic acid
RPX7009
UNII:1C75676F8V
vaborbactam
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