Nilofabicin

Nilofabicin (CG-400549) is an anti-bacterialagent that targets FabI. Nilofabicin shows high selectivity for the genus Staphylococcus and weak activity against most Gram-negative bacteria. Nilofabicin inhibits bacterial fatty acid biosynthesis, blocks phospholipid synthesis, and disrupts the structure of bacterial cell membranes. Nilofabicin exhibits in vivo antibacterial efficacy in a mouse model of systemic Staphylococcus aureus infection. Nilofabicin can be used in studies related to bacterial infections^[1][2][3]. In Vitro:Nilofabicin (CG-400549) exists in a total of 7 crystal forms, all of which exhibit excellent physical stability; they show different dissolution rates in artificial gastric juice at 37°C^[1].
Nilofabicin potently inhibits the growth of MSSA and MRSA isolates; experiments inducing drug resistance via fabI overexpression, as well as the identification of the F204L mutation in nilofabicin-resistant S. aureus, confirm that FabI is its primary target^[2].
Nilofabicin inhibits the growth of methicillin-resistant Staphylococcus aureus (MRSA) cells, with an MIC of 0.74 μM^[3]. In Vivo:Nilofabicin (CG400549) is a benzylpyridone that also exhibits potent activity against MSSA and MRSA isolates and is effective in combating systemic S. aureus infection in a murine model^[2].