Nafcillin Sodium Nafcillin sodium (CL 8491) reversibly inhibits β-lactamase with K d of 33 mM. In vitro
Nafcillin sodium inactivates β-lactamase through forming a covalent acyl-enzyme intermediate with β-lactamase via Ser-70. At concentrations above 80 mM, Nafcillin displays complete inhibition of β-lactamase within 200 s. Upon removal of the excess Nafcillin, the inhibited enzyme can be re-activated completely, with a rate constant of 2×10-3/s (25 ℃). Nafcillin sodium is activity against penicillin-resistant staphylococci. The minimal concentration necessary for antistaphylococcic activity in vitro ranges from 0.2 μg/mL to 2 μg/mL.