Cilastatin CAS 82009-34-5 is an inhibitor of renal peptidase. When used together with carbapenem antibiotics imine ligand, because of its specific inhibition of renal peptidase, it can prevent the latter from degradation of renal peptidase and improve the activity of imine ligand.

Cilastatin CAS 82009-34-5 is a synthetic inhibitor of dehydropeptidase I. Dehydropeptidase I is present in the brush margin of renal tubules. When imipenem enters the renal tubules, it is metabolized by the enzyme and loses its antimicrobial activity. Cilastatin CAS 82009-34-5 not only inhibits the metabolic action of this enzyme, but also prevents the production of possible nephrotoxic products. The mixture of Cilastatin CAS 82009-34-5 sodium and imipenem 1:1 is Tienan; Primaxin.

Imipenem cilastatin sodium not only has strong broad-spectrum antibacterial activity, but also inhibits β-lactamase. It is highly stable to β-lactamase and has strong antibacterial activity against negative bacilli. The antibacterial spectrum of imipenem cilastatin sodium includes almost all clinically significant pathogenic bacteria. Some group D streptococci are also sensitive to imipenem. It is widely used in patients with severe infection.