Cilastatin

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-beta-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 (Cay-15327). In a mouse model of systemic infection, cilastatin in combination with imipenem (Cay-16039) 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.Formal Name: (2Z)-7-[[(2R)-2-amino-2-carboxyethyl]thio]-2-[[[(1S)-2,2-dimethylcyclopropyl]carbonyl]amino]-2-heptenoic acid. CAS Number: 82009-34-5. Molecular Formula: C16H26N2O5S. Formula Weight: 358.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 12.5 mg/ml, DMSO: 12.5 mg/ml. SMILES: OC([C@@H](N)CSCCCC/C=C(C(O)=O)\NC([C@@H]1C(C)(C)C1)=O)=O. InChi Code: InChI=1S/C16H26N2O5S/c1-16(2)8-10(16)13(19)18-12(15(22)23)6-4-3-5-7-24-9-11(17)14(20)21/h6,10-11H,3-5,7-9,17H2,1-2H3,(H,18,19)(H,20,21)(H,22,23)/b12-6-/t10-,11+/m1/s1. InChi Key: DHSUYTOATWAVLW-WFVMDLQDSA-N.