SKU: R056  / 
    CAS Number: 1174020-13-3

    Relebactam Monohydrate

    3,529,500.00Rp - 10,823,800.00Rp

    Relebactam Monohydrate is a β-lactamase inhibitor that has the diazbicyclooctane core. It has a similar structure to avibactam. It has activity against a wide spectrum of β-lactamases including class A (extended-spectrum β-lactamases and KPC) and class C (AmpC) enzymes. The R1 side chain of Relebactam includes a piperidine ring. It can be used to inhibit the breakdown of certain compounds, such as the broad spectrum beta-lactam carbapenem antibiotic imipenem. Relebactam targets, binds to and inhibits beta-lactamase. This reduces the breakdown of compounds like imipenem, and thereby increases the activity and effect of such compounds that would otherwise be inactivated by beta-lactamase. The compound can be used in combination with imipenem (ie imipenem/cilastin/relebactam).

    Relebactam Monohydrate is soluble in DMSO.

    Molecular Formula C12H20N4O6S x H2O
    Mechanism of Action Relebactam is a diazabicyclooctane inhibitor with activity against a wide spectrum of β-lactamases.
    Microbiology Applications

    Relebactam is a non-β-lactam antimicrobial of the diazabicyclo[3.2.1]octanone (DBO) series. It inhibits most class A and class C β-lactamases, with selected inhibition of class D enzymes by avibactam.

    Relebactam inhibits 5 important class A serine B-lactamases (SBLs) representing both chromosomal and plasmid-borne enzymes (Tooke et al, 2019).

    Imipenem-Relebactam can be used against Enterobacteriaceae with complex β-lactamase backgrounds.

    Relebactam, when combined with imipenem, restores imipenem's activity against nonsusceptible isolates and enhances imipenem activity, specifically against susceptible Pseudomonas aeruginosa isolates.

    References

    Hilbert DW, DeRyke CA, Motyl M(2023) Relebactam restores susceptibility of resistant Pseudomonas aeruginosa and Enterobacterales and enhances imipenem activity against chromosomal AmpC-producing species: Analysis of global SMART 2018–2020. BMC Microbiol. 23:165

    Lang PA, Leissing TM, Page MGP, Schofield CJ, Brem J (2021) Structural investigations of the inhibition of Escherichia coli AmpC β-Lactamase by Diazabicyclooctanes. Antimicrob. Agents Chemother. 65(2):e02073-20 PMID 33199391

    Papp-Wallace KM et al (2018) Relebactam is a potent inhibitor of the KPC-2 β-Lactamase and restores imipenem susceptibility in KPC-producing Enterobacteriaceae. Antimicrob. Agents Chemother. 62(6):e00174-18. PMID: 29610205

    Tooke CL et al (2019) Molecular basis of class A β-lactamase inhibition by Relebactam. Antimicrobial Agents Chemother. 63(10):e00564-1