Cilastatin (MK0791)

An inhibitor of dipeptidase (dehydropeptidase I)

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库存: 现货

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数量
10mg

￥537.00

430.00

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50mg

￥975.00

780.00

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100mg

￥1512.00

1210.00

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Background

Cilastatin is an inhibitor of dipeptidase (dehydropeptidase I), a renal dipeptidase.¹ It inhibits human renal dipeptidase (K_i = 0.7 μM), porcine dipeptidase (IC₅₀ = 0.11 μM), and bacterial metallo-β-lactamase CphA from A. hydrophila (IC₅₀ = 178 μM).^1,2,3 Cilastatin (200 μg/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.

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., Cama?o, S., et al.Protective effects of cilastatin against vancomycin-induced nephrotoxicityBiomed Res. Int.704382(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)