| 规格: | 98% |
| 分子量: | 362.5 |
| 包装 | 价格(元) |
| 500ug | 电议 |
| 1mg | 电议 |
Background:
Cilastatin-15N-d3is intended for use as an internal standard for the quantification of cilastatin by GC- or LC-MS. Cilastatin is an inhibitor of dipeptidase (dehydropeptidase I), a renal dipeptidase.1It inhibits human renal dipeptidase (Ki= 0.7 μM), porcine dipeptidase (IC50= 0.11 μM), and bacterial metallo-β-lactamase CphA fromA. hydrophila(IC50= 178 μM).1,2,3Cilastatin (200 μg/ml) protects primary porcine renal proximal tubular epithelial cells from nephrotoxicity and apoptosis induced by vancomycin .4In a mouse model of systemic infection, cilastatin in combination with imipenem protects mice fromS. aureus,E. coli, andP. aeruginosainfection.5Cilastatin was designed to inhibit renal metabolism of imipenem and prolong its half-life.2Formulations containing cilastatin in combination with imipenem have been used to treat susceptible bacterial infections.
1.Campbell, B.J., Forrester, L.J., Zahler, W.L., et al.Beta-lactamase activity of purified and partially characterized human renal dipeptidaseJ. Biol. Chem.259(23)14586-14590(1984) 2.Kahan, F.M., Kropp, H., Sundelof, J.G., et al.Thienamycin: Development of imipenen-cilastatinJ. Antimicrob. Chemother.12(Suppl. D)1-35(1983) 3.Keynan, S., Hooper, N.M., Felici, A., et al.The renal membrane dipeptidase (dehydropeptidase I) inhibitor, cilastatin, inhibits the bacterial metallo-β-lactamase enzyme CphAAntimicrob. Agents Chemother.39(7)1629-1631(1995) 4.Humanes, B., Jado, J.C., CamaÑo, S., et al.Protective effects of cilastatin against vancomycin-induced nephrotoxicityBiomed Res. Int.2015704382(2015) 5.Petersen, P.J., Jacobus, N.V., Weiss, W.J., et al.In vitro and in vivo activities of LJC10,627, a new carbapenem with stability to dehydropeptidase IAntimicrob. Agents Chemother.35(1)203-207(1991)
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