Beta-lactamase Inhibitor

Lalistat 1 is a potent, selective, and competitive inhibitor of lysosomal acid lipase (LAL) and against purified human LAL (phLAL) with an IC₅₀ of 68 nM. Lalistat 1 is a inhibitor of immunoglobulin A1 protease (IgA1P) proteases for H. influenzae, has less effects on other serine hydrolases (trypsin or β-lactamase, etc.). Lalistat 1 can be used for the research of niemann-pick type C (NPC) disease.

Enmetazobactam (AAI101) is an extended-spectrum β-lactamase inhibitor, against many resistant Gram-negative pathogens.

Avibactam sodium (NXL-104) hydrate 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.

Cefuroxime sodium is an orally active second-generation cephalosporin antibiotic with increased stability to β-lactamase. Cefuroxime sodium has a broad spectrum activity against Gram-positive and Gram-negative bacteria.

Thiamphenicol (Thiophenicol), a methyl-sulfonyl derivative of Chloramphenicol, is a broad-spectrum antimicrobial antibiotic. Thiamphenicol acts by binding to the 50S ribosomal subunit, leading to inhibition of protein synthesis and bacteriostatic effect (against Gram-negative, Gram-positive aerobic and anaerobic bacteria).

Nacubactam (OP0595 free acid) is a potent non-β-lactam-β-lactamase inhibitor with activity against class A and C β-lactamases. Nacubactam acts as a penicillin binding protein (PBP) 2-active antibacterial, and gives β-lactamase-independent potentiation of β-lactams targeting other PBPs. Nacubactam potentiates the antimicrobial activities of Piperacillin (HY-B1923), Cefepime (HY-B0692), and Meropenem (HY-13678) against CTX-M-15-positive Escherichia coli and KPC-positive Klebsiella pneumoniae.

Ceftibuten (Sch-39720) dihydrate, an antibiotic, is an orally active cephalosporin, possesses potent activity in vitro against a wide range of gram-negative and certain gram-positive pathogens.

Cefuroxime is an orally active second-generation cephalosporin antibiotic with increased stability to β-lactamase. Cefuroxime has a broad spectrum activity against Gram-positive and Gram-negative bacteria.

Nafcillin sodium monohydrate, an antibiotic, is a reversible inhibitor of β-lactamase. Nafcillin sodium monohydrate can be used for the research of staphylococcal infections.

Ceftazidime (GR20263) pentahydrate , an antibiotic, has a broad spectrum activity against Gram-positive and Gram-negative aerobic bacteria. Ceftazidime pentahydrate is also active against Enterobacteriaceae (including β-lactamase-positive strains) and is resistant to hydrolysis by most β-lactamases.

Taniborbactam (VNRX-5133) is a reversible and selective boronic acid-containing pan-spectrum β-lactamase inhibitor with IC₅₀s of 8-530 nM. Taniborbactam has IC₅₀s of 30 nM, 32 nM, 42 nM, 20 nM for KPC-2, AmpC, OXA-48, and VIM-2. Taniborbactam is against Gram-negative bacteria.

Moxalactam (Latamoxef) sodium salt is a synthetic oxa-β-lactam antibiotic. Moxalactam sodium salt has a broad spectrum of activity against Gram-positive and Gram-negative aerobic and anaerobic bacteria. Moxalactam sodium salt inhibits production of β-lactamases.

Sulopenem (CP-70429) is an orally active, parenteral penem antibiotic with broad-spectrum activities against Gram-positive and Gram-negative bacteria. Sulopenem has the potential for urinary tract infections and intra-abdominal infections treatment. Sulopenem is inactive against Pseudomonas aeruginosa and Xanthomonas maltophilia.

Cibacron Blue 3G-A is an anthraquinone dye, inhibits the R46 β-lactamase with a K_i value of 1.2 uM.

Cloxacillin sodium is an orally active antibacterial agent and β-lactamase inhibitor with an IC₅₀ of 0.04 µM. Cloxacillin sodium can suppress the S. aureus-induced inflammatory response by inhibiting the activation of MAPKs, NF-кB and NLRP3-related proteins.

Pilabactam (ANT3310) sodium is a broad-spectrum covalent Serine β-Lactamase inhibitor, with IC₅₀ values ranging from 1 nM to 175 nM (a panel of Serine β-Lactamase). Pilabactam sodium potentiates activity of β-lactam antibiotics against Carbapenem-Resistant Enterobacterales (CRE) and Acinetobacter baumannii (CRAB). Pilabactam sodium can be used in the research of bacterial infection.

Biapenem (CLI 86815; L 627; LJC 10627) a parenteral carbapenem antibacterial agent with a broad spectrum.

Avibactam (NXL-104) free acid 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.

Cloxacillin sodium monohydrate is an orally active antibacterial agent and β-lactamase inhibitor with an IC₅₀ of 0.04 µM. Cloxacillin sodium monohydrate can suppress the S. aureus-induced inflammatory response by inhibiting the activation of MAPKs, NF-кB and NLRP3-related proteins.

Cefonicid sodium is a long-acting cephalosporin antibiotic. Cefonicid sodium also acts as a noncompetitive class I β-lactamase inhibitor with a K_i value of 0.8 μM. Cefonicid sodium exhibits broad-spectrum antimicrobial activity and is effective against a variety of Gram-positive and Gram-negative bacteria. Cefonicid sodium can be used for research on infections.