Introduction：Basic information about CAS 1360457-46-0|Vaborbactam, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Vaborbactam |
|---|
| CAS Number | 1360457-46-0 | Molecular Weight | 297.135 |
|---|
| Density | 1.4±0.1 g/cm3 | Boiling Point | / |
|---|
| Molecular Formula | C12H16BNO5S | Melting Point | / |
|---|
| MSDS | / | Flash Point | / |
|---|
Names
| Name | vaborbactam |
|---|
| Synonym | More Synonyms |
|---|
Vaborbactam BiologicalActivity
| Description | Vaborbactam is a cyclic boronic acid pharmacophore β-lactamase inhibitor. |
|---|
| Related Catalog | Signaling Pathways >>Anti-infection >>BacterialResearch Areas >>Infection |
|---|
| 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 |
