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1360457-46-0

1360457-46-0 structure
1360457-46-0 structure
  • Name: Vaborbactam
  • Chemical Name: vaborbactam
  • CAS Number: 1360457-46-0
  • Molecular Formula: C12H16BNO5S
  • Molecular Weight: 297.135
  • Catalog: Signaling Pathways Anti-infection Bacterial
  • Create Date: 2018-05-20 08:00:00
  • Modify Date: 2024-01-02 20:18:06
  • Vaborbactam is a cyclic boronic acid pharmacophore β-lactamase inhibitor.

Name vaborbactam
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
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.

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℃