ANT3310 sodium

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). ANT3310 sodium potentiates activity of β-lactam antibiotics against Carbapenem-Resistant Enterobacterales (CRE) and Acinetobacter baumannii (CRAB). ANT3310 sodium can be used in the research of bacterial infection[1][2].

Research Areas >> Infection

Signaling Pathways >> Anti-infection >> Bacterial

ANT3310 sodium (Compound 21, 0.006 to 3 000 nM, 10 min) inhibits a series of Serine β-Lactamase (AmpC, CTX-M-15, TEM-1, OXA-48, OXA-23, and KPC-2), with IC<>50 values ranging from 1 nM to 175 nM[1]. ANT3310 sodium shows a low in vitro cytotoxicity (IC<>50: > 100 μM) in HepG2 cell, cardiotoxicity (inhibition of the hERG potassium ion channel), and genotoxicity (Ames test)[1].

ANT3310 sodium (intravenous injection, 25-100 mg/kg, at 1, 3, 5, and 7 h postinfection) reduces bacterial burdens in murine thigh infection model[1]. ANT3310 sodium (intravenous injection, 1 mg/kg, Male Swiss albino mice) shows a T1/2 value of 0.64 h, AUC value of 412 ng•h/mL, and Cl value of 40 mL/min/kg (pharmacokinetic assay)[1]. Animal Model: Murine thigh infection model[1] Dosage: 25, 50, and 100 mg/kg Administration: Intravenous injection, at 1, 3, 5, and 7 h postinfection Result: Reduced bacterial burdens (colony forming units, CFU) in a dose-dependent manner to levels below that of the initial starting inoculum at the highest dose, when treated with the combination of MEM.

[1]. David T Davies, et al. Discovery of ANT3310, a Novel Broad-Spectrum Serine β-Lactamase Inhibitor of the Diazabicyclooctane Class, Which Strongly Potentiates Meropenem Activity against Carbapenem-Resistant Enterobacterales and Acinetobacter baumannii. J Med Chem. 2020 Dec 24;63(24):15802-15820.