Relebactam is a diazabicyclooctane inhibitor with activity against a wide spectrum of β-lactamases, including class A (extended-spectrum β-lactamases [ESBLs] and KPC) and class C (AmpC) enzymes.Target: beta-lactamaseImipenem with Relebactam is active against Escherichia coli, Klebsiella pneumoniae, and Enterobacter spp., including K. pneumoniae carbapenemase (KPC)-producing isolates. The combination of Imipenem with Relebactam demonstrated activity against KPC-producing Enterobacteriaceae and multidrug-resistant P. aeruginosa. The imipenem MIC50 and MIC90 values for the ESBL-producing isolates were 0.25 and 0.5 μg/ml, respectively; with the addition of Relebactam, the corresponding values were 0.25 and 0.25 μg/ml. Five isolates harbored blaKPC. For these 5 isolates, the imipenem MICs ranged from 0.5 to >32 μg/ml. With the addition of Relebactam, the MICs decreased to 0.12 to 0.5 μg/ml. Relebactam inhibits most class A and class C β-lactamases, with selected inhibition of class D enzymes by avibactam. β-Lactamase inhibitors (BLIs) have played an important role in combatting β-lactam resistance in Gram-negative bacteria, but their effectiveness has diminished with the evolution of diverse and deleterious varieties of β-lactamases.

Product information

CAS Number: 1174018-99-5

Molecular Weight: 348.38

Formula: C12H20N4O6S

Chemical Name: [(1R,2S,5R)-7-oxo-2-[(piperidin-4-yl)carbamoyl]-1,6-diazabicyclo[3.2.1]octan-6-yl]oxidanesulfonic acid

Smiles: OS(=O)(=O)ON1[C@H]2C[N@]([C@@H](CC2)C(=O)NC2CCNCC2)C1=O

InChiKey: SMOBCLHAZXOKDQ-ZJUUUORDSA-N

InChi: InChI=1S/C12H20N4O6S/c17-11(14-8-3-5-13-6-4-8)10-2-1-9-7-15(10)12(18)16(9)22-23(19,20)21/h8-10,13H,1-7H2,(H,14,17)(H,19,20,21)/t9-,10+/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: H2O : 50 mg/mL (143.52 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.