β-lactamase

Xeruborbactam is a potent boronic acid beta-lactamase inhibitor that targets both serine and metallo beta-lactamases with high efficacy. Demonstrating activity in the nanomolar range, it serves as an ultra-broad-spectrum agent in combating antibiotic resistance. Xeruborbactam is valuable for research applications focused on understanding beta-lactamase activity and developing novel antimicrobial strategies.

Metallo-β-lactamase-IN-7 is a specific inhibitor of VIM-type metallo-β-lactamases, demonstrating potent inhibition with IC50 values of 0.019 μM for VIM-2, 13.64 μM for VIM-1, and 0.38 μM for VIM-5. This compound enhances the antibacterial efficacy of Meropenem against Gram-negative bacterial strains, making it a valuable tool in combating antibiotic resistance in microbial research. Its application is crucial for studies focused on understanding and overcoming metallo-β-lactamase mediated resistance mechanisms.

β-Lactamase-IN-4 is a potent β-lactamase inhibitor that targets β-lactamase enzymes, effectively enhancing the efficacy of β-lactam antibiotics. This compound is critical for research applications focused on combating bacterial infections caused by β-lactamase-producing microorganisms. Its use may contribute to the development of novel therapeutic strategies against resistant bacterial strains.

Metallo-β-lactamase-IN-6 is a potent inhibitor of VIM-type metallo-β-lactamases, demonstrating IC50 values of 0.56 μM for VIM-2, 29.50 μM for VIM-1, and 5.78 μM for VIM-5. This compound exhibits significant antibacterial synergy with Meropenem against engineered Escherichia coli strains and clinically isolated Pseudomonas aeruginosa strains that produce VIM-2 metallo-β-lactamase. It serves as a valuable research tool for exploring resistance mechanisms in bacterial pathogens and for developing novel therapeutic strategies.

FPI-1602 is a β-lactamase inhibitor that enhances the efficacy of β-lactam antibiotics. It exhibits significant antimicrobial activity against pathogens such as Pseudomonas aeruginosa, Escherichia coli, and Enterobacter spp. This compound is valuable for research applications aimed at overcoming antibiotic resistance mediated by β-lactamase enzymes.

Brobactam is a potent synthetic β-lactamase inhibitor designed to combat antibiotic resistance by inhibiting β-lactamase enzymes. It exhibits broad-spectrum antibacterial activity, making it valuable in the study and treatment of β-lactamase-mediated resistance in various bacterial infections. Research applications include the evaluation of combination therapies and the development of novel antibacterial agents.

KSP-1007 is a bicyclic boronate compound functioning as a broad-spectrum β-lactamase inhibitor. It effectively targets class A, B, C, and D β-lactamases, including serine-type and metallo-type enzymes such as NDM, VIM, and IMP, in addition to Acinetobacter baumannii OXA-type enzymes. KSP-1007 enhances the antibacterial activity of Meropenem, decreasing its minimum inhibitory concentration (MIC) against carbapenemase-producing Enterobacteriaceae, Acinetobacter baumannii, and Pseudomonas aeruginosa. This reagent is suitable for research on bacterial infections and antibiotic resistance mechanisms.

Ledaborbactam etzadroxil is an orally active inhibitor of Ambler class A, C, and D β-lactamase enzymes. It is designed to provide enhanced protection for β-lactam antibiotics from hydrolysis by these enzymes, thereby improving their efficacy. This compound is particularly relevant in research applications focused on combating antibiotic resistance and expanding the therapeutic options for bacterial infections.

β-Lactamase-IN-8 is a potent β-lactamase inhibitor with a broad-spectrum profile, utilizing a cyclic boronate structure to enhance oral bioavailability. It effectively inhibits various β-lactamases, making it a valuable tool for studying antibacterial resistance mechanisms and developing new therapeutic strategies against resistant bacterial strains. Researchers can utilize β-Lactamase-IN-8 for investigating the efficacy of β-lactam antibiotics in microbial infections.

β-Lactamase-IN-7 is a potent inhibitor of VIM-type metallo-β-lactamases, exhibiting inhibition constants (Ki) of 1.26 μM and 0.54 μM for VIM-1 and VIM-4, respectively. This compound demonstrates effective inhibition against Klebsiella pneumoniae, making it valuable for studies focused on antibiotic resistance and the development of novel therapeutic strategies against resistant bacterial infections. Its role in characterizing metallo-β-lactamase activity positions it as an important tool in chemical biology research.

Durlobactam, also known as ETX2514, is a beta-lactamase inhibitor drug candidate.

Avibactam sodium (NXL-104) is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively.

AAI-101, also known as Enmetazobactam, is a beta lactamase inhibitor potentially for the treatment of multi-drug resistant gram-negative bacterial infections.

Zidebactam sodium salt (WCK-5107 sodium salt) is a potent β-lactamase inhibitor. Zidebactam also is a penicillin-binding protein2 (PBP2) inhibitor with an IC50 of 0.26 μg/mL.

Sulopenem (CP-70429) is an orally active, potent inhibitor of beta-lactamase. Sulopenem is a parenteral penem antibiotic with broad-spectrum activities against Gram-positive and Gram-negative bacteria.

Vaborbactam is a cyclic boronic acid pharmacophore β-lactamase inhibitor.

BRL-42715 is a potent inhibitor of a broad range of bacterial beta-lactamases (β-lactamase) .

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.

Taniborbactam is a potent inhibitor of β-lactamase, with IC50s of <100 nM for SHV-5, KPC-2, VIM-2, and AmpC β-lactamase, and 0.1 to 1 μM for OXA-1 β-lactamase, used in the research of bacterial infections.

Zidebactam (WCK-5107) is a potent β-lactamase inhibitor. Zidebactam also is a penicillin-binding protein2 (PBP2) inhibitor with an IC50 of 0.26 μg/mL.

VNRX-5133 is a cyclic boronate β-lactamase inhibitor.

Nacubactam (OP0595 free acid) is a potent non-β-lactam-β-lactamase inhibitor with activity against class A and class C β-lactamases.

RDR 02308 is a β-lactamase inhibitor that targets the TLR4-MyD88 signaling pathway. This compound effectively inhibits the activity of full-length β-lactamase, providing a valuable tool for studies related to antibiotic resistance. Its mechanism of action makes it suitable for research applications focused on bacterial infections and the development of novel therapeutic strategies.