ANT3310 is a broad-spectrum covalent inhibitor of serine β-lactamase (Serine β-Lactamase) with an IC50 range of 1 nM to 175 nM against various serine β-lactamases. ANT3310 enhances the efficacy of β-lactam antibiotics against carbapenem-resistant Enterobacteriaceae (CRE) and carbapenem-resistant Acinetobacter baumannii (CRAB). It is applicable for studies related to bacterial infections.

Pilabactam (Compound 21, 0.006-3,000 nM, 10 minutes) effectively inhibits a range of serine β-lactamases, including AmpC, CTX-M-15, TEM-1, OXA-48, OXA-23, and KPC-2, with IC50 values from 1 nM to 175 nM. It demonstrates low in vitro cytotoxicity (IC50: >100 μM), cardiotoxicity (inhibition of hERG potassium channel), and genotoxicity (Ames test) in HepG2 cells.

Pilabactam, when administered intravenously at doses of 25-100 mg/kg at 1, 3, 5, and 7 hours post-infection, reduces bacterial load in a mouse thigh infection model. For pharmacokinetic assessment, Pilabactam (intravenous injection, 1 mg/kg, male Swiss albino mice) exhibits a half-life (T 1/2) of 0.64 hours, an area under the curve (AUC) of 412 ng•h/mL, and a clearance (Cl) rate of 40 mL/min/kg.