Sulopenem

Sulopenem (CAS 120788-07-0) is a broad-spectrum penem antibiotic developed by Pfizer with potent activity against gram-positive, gram-negative, and anaerobic pathogens, also known as PF-06273095 and CP-70429. The compound is notable for its stability against β-lactamases and renal dehydropeptidase I, making it a relevant research tool in antimicrobial resistance studies. Enamine offers Sulopenem as a high-purity screening sample for microbiology and translational research applications.

Sulopenem (CAS 120788-07-0)

Sulopenem molecular weight is 349.43 g/mol, with molecular formula C₁₂H₁₅NO₅S₃. The Sulopenem chemical structure belongs to the penem class of β-lactam antibiotics, combining structural elements of penicillins, cephalosporins, and carbapenems within a bicyclic thiazetidine ring system. The Sulopenem structure features a hydroxyethyl side chain at C-6 and a thiolanyl sulfoxide substituent at C-3, the latter conferring enhanced β-lactamase stability. Researchers examine the Sulopenem Pfizer development data alongside structural analysis to study penem scaffold optimization and PBP binding selectivity. The compound is registered under CAS 120788-07-0 and is available as both parenteral and oral prodrug formulations.

Application Sulopenem

Sulopenem is applied in antimicrobial research targeting multidrug-resistant (MDR) Enterobacterales, ESBL-producing pathogens, and anaerobic bacterial infections. As a PF-06273095 reference compound, it is used in susceptibility testing against urinary tract and intra-abdominal infection isolates, including fluoroquinolone-resistant and carbapenem-comparator strains. Sulopenem Pfizer clinical datasets from Phase 2 and Phase 3 trials in complicated and uncomplicated UTIs make it particularly relevant for translational antibiotic research and antimicrobial stewardship studies. The compound also serves as a structural comparator in β-lactam scaffold optimization programs.

Biochemical and Physiological Actions

Sulopenem exerts bactericidal activity by binding to penicillin-binding proteins, particularly PBP1a, PBP1b, PBP2, and PBP3 in E. coli, inhibiting peptidoglycan cross-linking and triggering cell lysis. Unlike many β-lactams, the Sulopenem structure confers intrinsic stability against hydrolysis by a broad range of β-lactamases, including ESBL and AmpC enzymes, without requiring a co-administered inhibitor. The compound also demonstrates natural stability against renal dehydropeptidase I, eliminating the need for cilastatin co-administration. Bactericidal efficacy follows a time-dependent pharmacodynamic pattern, with bacteriostasis linked to %fT>MIC values of 8.6–17% and 2-log₁₀ kill achieved at 12–28% in murine infection models.

Features and Benefits Sulopenem

Sulopenem (PF-06273095, CAS 120788-07-0) offers a well-characterized antibacterial profile for antimicrobial and resistance research:

• broad-spectrum activity covering ESBL-producing Enterobacterales, gram-positive, and anaerobic pathogens at MIC ≤1 µg/mL;
• intrinsic β-lactamase stability without requirement for a co-administered inhibitor;
• dehydropeptidase I stability enabling standalone parenteral and oral prodrug dosing;
• Phase 2 and Phase 3 clinical datasets available for translational reference.