Prevents renal metabolism of penem and carbapenem antibiotics by specific and reversible dehydropeptidase I inhibition. Antibacterial adjunct. Cilastatin is an inhibitor of dipeptidase (dehydropeptidase I), a renal dipeptidase.1 It inhibits human renal dipeptidase (Ki = 0.7uM), porcine dipeptidase (IC50 = 0.11uM), and bacterial metallo-beta-lactamase CphA from A. hydrophila (IC50 = 178uM).1,2,3 Cilastatin (200ug/ml) protects primary porcine renal proximal tubular epithelial cells from nephrotoxicity and apoptosis induced by vancomycin.4 In a mouse model of systemic infection, cilastatin in combination with imipenem protects mice from S. aureus, E. coli, and P. aeruginosa infection.5 Cilastatin was designed to inhibit renal metabolism of imipenem and prolong its half-life.2 Formulations containing cilastatin in combination with imipenem have been used to treat susceptible bacterial infections. Synonyms: (2Z)-7-[[(2R)-2-amino-2-carboxyethyl]thio]-2-[[[(1S)-2,2-dimethylcyclopropyl]carbonyl]amino]-2-heptenoic Acid, MK-791 CAS No: 82009-34-5 Molecular Formula: C16H26N2O5S Molecular Weight: 358.45 Appearance: Supplied to white to light brown solid Purity: ~98% Solubility: DMSO, Methanol Melting Point: 143-146C (dec) Method for Determining Identity: Proton NMR (DMSO-d6), Spectroscopic and Mass Spectrometric Analysis TLC Conditions: C18, Acetonitrile: Water Acetic Acid,=8:1:0.15, Visualized with UV and AMCS, Rf=0.55 Storage and Stability: May be stored at RT for short-term only. Long-term storage is recommended at -20C. Stable for 6 months after receipt. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Important Note: This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological. Toxicity and Hazards: All products should be handled by qualified personnel only, trained in laboratory procedures.
Molecular Weight:
358.45
Purity:
~98%
Form:
Supplied as an off-white solid to pale yellow solid
CAS Number:
[82009-34-5]
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