Nacubactam

• CAT Number: I008221
• CAS Number: 1452458-86-4
• Molecular Formula: C9H16N4O7S
• Molecular Weight: 324.31
• Purity: ≥95%
• Synonyms: Nacubactam; RG-6080; RG 6080; RG6080; FPI-1459; FPI 1459; FPI1459; OP-0595; OP 0595; OP0595;(1R,2S,5R)-2-((2-aminoethoxy)carbamoyl)-7-oxo-1,6-diazabicyclo[3.2.1]octan-6-yl hydrogen sulfate
• Target: Beta-lactamase
• Solubility: Soluble in DMSO
• Storage: 0 - 4 °C for short term, or -20 °C for long term
• IUPAC Name: [(2S,5R)-2-(2-aminoethoxycarbamoyl)-7-oxo-1,6-diazabicyclo[3.2.1]octan-6-yl] hydrogen sulfate
• InChI: InChI=1S/C9H16N4O7S/c10-3-4-19-11-8(14)7-2-1-6-5-12(7)9(15)13(6)20-21(16,17)18/h6-7H,1-5,10H2,(H,11,14)(H,16,17,18)/t6-,7+/m1/s1
• InChIKey: RSBPYSTVZQAADE-RQJHMYQMSA-N
• SMILES: C1C[C@H](N2C[C@@H]1N(C2=O)OS(=O)(=O)O)C(=O)NOCCN

Nacubactam (Cat No.:I008221) is a potent beta-lactamase inhibitor that enhances the activity of beta-lactam antibiotics against multidrug-resistant bacteria. By targeting and inhibiting various classes of beta-lactamases, enzymes responsible for antibiotic resistance, nacubactam restores the effectiveness of beta-lactam antibiotics. This compound shows promise in combating drug-resistant Gram-negative bacteria, including those resistant to carbapenems. Nacubactam, when used in combination with beta-lactam antibiotics, has potential applications in the treatment of infections caused by drug-resistant bacteria, offering a new therapeutic option in the fight against antibiotic resistance.

Overview of Clinical Research

Nacubactam  is a beta-lactamase inhibitor developed by Roche. The clinical trials in Bacterial infections (In volunteers) initiated in Japan (IV) before October 2020.

Reference

1.Monogue, Marguerite L., et al. "In vivo efficacy of meropenem with a novel non-β-lactam–β-lactamase inhibitor, nacubactam, against Gram-negative organisms exhibiting various resistance mechanisms in a murine complicated urinary tract infection model." Antimicrobial agents and chemotherapy 62.9 (2018).
2.Barnes, Melissa D., et al. "Nacubactam enhances meropenem activity against carbapenem-resistant Klebsiella pneumoniae producing KPC." Antimicrobial agents and chemotherapy 63.8 (2019): e00432-19.