Vaborbactam

Vaborbactam is an inhibitor of beta-lactamases (Kis = 29-110 nM for class A and class C enzymes). It is selective for bacterial beta-lactamases over a panel of mammalian serine proteases (IC50s = >1,000 µM). Vaborbactam potentiates the activity of biapenem against K. pneumonia expressing the beta-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 (Cay-16068), ertapenem, and imipenem (Cay-16039) against clinical isolates of E. coli, E. cloacae, K. oxytoca, and K. pneumoniae that produce serine beta-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.Formal Name: 2-hydroxy-3R-[[2-(2-thienyl)acetyl]amino]-1,2-oxaborinane-6S-acetic acid. CAS Number: 1360457-46-0. Synonyms: RPX 7009. Molecular Formula: C12H16BNO5S. Formula Weight: 297.1. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, Ethanol: 10 mg/ml, PBS (pH 7.2): 1 mg/ml. lambdamax: 202, 233 nm. SMILES: OB1O[C@H](CC(O)=O)CC[C@@H]1NC(CC2=CC=CS2)=O. InChi Code: InChI=1S/C12H16BNO5S/c15-11(7-9-2-1-5-20-9)14-10-4-3-8(6-12(16)17)19-13(10)18/h1-2,5,8,10,18H,3-4,6-7H2,(H,14,15)(H,16,17)/t8-,10-/m0/s1. InChi Key: IOOWNWLVCOUUEX-WPRPVWTQSA-N.