A β-lactamase inhibitor (Kis = 29-110 nM for class A and class C enzymes); selective for bacterial β-lactamases over a panel of mammalian serine proteases (IC50s = ≥1

Vaborbactam – 5 mg

Brand:
Cayman
CAS:
1360457-46-0
Storage:
-20
UN-No:
Non-Hazardous - /

Vaborbactam is an inhibitor of β-lactamases (Kis = 29-110 nM for class A and class C enzymes).{36683} It is selective for bacterial β-lactamases over a panel of mammalian serine proteases (IC50s = ≥1,000 μM). Vaborbactam potentiates the activity of biapenem against K. pneumonia expressing the β-lactamase KPC-2, reducing the MIC value for biapenem from 32 to 1 μg/ml when used at a concentration of 0.02 μg/ml. It also potentiates the activity of the carbapenem antibiotics biapenem, meropenem (Item No. 16068), ertapenem, and imipenem (Item No. 16039) against clinical isolates of E. coli, E. cloacae, K. oxytoca, and K. pneumoniae that produce serine β-lactamases (MICs = ≤0.06-4 and 4-64 μg/ml in the presence and absence of vaborbactam, respectively). In vivo, vaborbactam (50 mg/kg) reduces the number of colony forming units (CFUs) in the lung in a neutropenic mouse lung infection model when used in combination with biapenem or meropenem. Formulations containing vaborbactam in combination with meropenem have been used for the treatment of carbapenem-resistant Enterobacteriaceae infections.  

 

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Description

A β-lactamase inhibitor (Kis = 29-110 nM for class A and class C enzymes); selective for bacterial β-lactamases over a panel of mammalian serine proteases (IC50s = ≥1,000 μM); potentiates the activity of biapenem against K. pneumonia expressing KPC-2 at 0.02 μg/ml; potentiates the activity of carbapenem antibiotics against clinical isolates of various bacteria (MICs = ≤0.06-4 and 4-64 μg/ml in the presence and absence of compound, respectively); reduces the number of CFUs in the lung in a neutropenic mouse lung infection model when used in combination with biapenem or meropenem at 50 mg/kg

Formal name: 2-hydroxy-3R-[[2-(2-thienyl)acetyl]amino]-1,2-oxaborinane-6S-acetic acid

Synonyms:  RPX 7009

Molecular weight: 297.1

CAS: 1360457-46-0

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Immunology & Inflammation||Research Area|Infectious Disease|Bacterial Diseases|Pneumonia

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