Pilabactam  (Synonyms: ANT3310)

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

Pilabactam (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 IC₅₀ values ranging from 1 nM to 175 nM^[1].
Pilabactam 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pilabactam (intravenous injection, 25-100 mg/kg, at 1, 3, 5, and 7 h postinfection) reduces bacterial burdens in murine thigh infection model^[1].
Pilabactam (intravenous injection, 1 mg/kg, Male Swiss albino mice) shows a T_1/2 value of 0.64 h, AUC value of 412 ng•h/mL, and Cl value of 40 mL/min/kg (pharmacokinetic assay)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

240.21

C₆H₉FN₂O₅S

2410688-60-5

O=S(ON1[C@H]2C[N@]([C@@H](CC2)F)C1=O)(O)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]