A neuropeptide with diverse biological activities
货号:ajcx22084
CAS:N/A
分子式:C16H23D3N[15N]O5S
分子量：362.5
溶解度:DMSO: Soluble,Methanol: Soluble,Water: Soluble
纯度：98%
存储：Store at -20°C
库存：现货

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 (K_i= 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)