Product Name:    Cilastatin

Synonyms:    Cilistatin Acid;(z)-7-[(2s)-2-amino-3-hydroxy-3-oxopropyl]sulfanyl-2-[[(1s)-2,2-dimethylcyclopropanecarbonyl]amino]hept-2-enoic acid;(r-(r*,s*-(z)))-)carbonyl)amino);mk-791;CILASTATIN;Cilastain;(2Z)-7-[[(2R)-2-amino-2-carboxyethyl]thio]-2-[[[(1S)-2,2-dimethylcyclopropyl]carbonyl]amino]-2-heptenoic Acid;Cilastatin acid

CAS:    82009-34-5

MF:    C16H26N2O5S

MW:    358.45

EINECS:    279-875-8

Product Categories:    Inhibitors;Chiral Reagents;Intermediates & Fine Chemicals;Pharmaceuticals

Cilastatin is an inhibitor of dipeptidase (dehydropeptidase I), a renal dipeptidase. It inhibits human renal dipeptidase (Ki = 0.7 μM), porcine dipeptidase (IC50 = 0.11 μM), and bacterial metallo-β-lactamase CphA from A. hydrophila (IC50 = 178 μM). Cilastatin (200 μg/ml) protects primary porcine renal proximal tubular epithelial cells from nephrotoxicity and apoptosis induced by vancomycin . In a mouse model of systemic infection, cilastatin in combination with imipenem protects mice from S. aureus, E. coli, and P. aeruginosa infection. Cilastatin was designed to inhibit renal metabolism of imipenem and prolong its half-life. Formulations containing cilastatin in combination with imipenem have been used to treat susceptible bacterial infections.